Absorption, Distribution and Excretion
The pharmacokinetics of gadodiamine administered intravenously in normal subjects conformed to an open two-compartment model. Gadodiamine is primarily excreted in the urine, with 95.4 ± 5.5% (mean ± standard deviation) of the administered dose being excreted within 24 hours. The volume of distribution of gadodiamine (200 ± 61 mL/kg) is comparable to that of extracellular fluid. After administration of gadolinium-based contrast agents (GBCAs), gadolinium can remain in the brain, bone, skin, and other organs for months or even years. The renal and plasma clearances of gadodiamine are nearly identical (1.7 and 1.8 mL/min/kg, respectively), similar to substances primarily excreted via glomerular filtration. This study aimed to determine the residual gadolinium (Gd) concentration in human bone tissue after administration of standard clinical doses of two gadolinium-based contrast agents (ProHance and Omniscan). Bone specimens were collected and analyzed after patients undergoing hip replacement surgery were injected with 0.1 mmol/kg gadolinium chelate, and compared with an age-matched control group without a history of gadolinium chelate injection. Bone specimens were freshly collected, refrigerated, and then frozen. After grinding and freeze-drying, tissue digestion was performed using a polytetrafluoroethylene digestion vessel and concentrated nitric acid. This study developed and validated a method for analyzing gadolinium content in bone samples using inductively coupled plasma mass spectrometry (ICP-MS). The results were compared with a previous study analyzing the same tissue samples using different techniques. ICP-MS showed a tissue gadolinium retention of 1.77 ± 0.704 μg Gd/g bone (n=9) as measured by Omniscan and 0.477 ± 0.271 μg Gd/g bone (n=10) as measured by ProHance. These results are consistent with previous ICP-AES studies. Compared to ProHance (Gd[HP-DO3A]), Omniscan (Gd[DTPA-BMA]) left approximately four times more gadolinium residue in bone (previous studies reported 2.5 times). Twenty-seven patients—nine with severely impaired renal function (glomerular filtration rate 2–10 mL/min), nine on hemodialysis, and nine on continuous ambulatory peritoneal dialysis—were followed for 5, 8, and 22 days, respectively, after receiving gadodiamine injection (0.1 mmol/kg body weight). Gadodiamine injection did not cause changes in renal function. In patients with severely impaired renal function, the elimination half-life of gadodiamine injection (34.3 hours ± 22.9 hours) was prolonged compared to healthy volunteers (1.3 hours ± 0.25 hours). On average, 65% of the injected gadodiamine was cleared during a single hemodialysis session. Following 22 days of continuous ambulatory peritoneal dialysis, 69% of the total gadodiamine was eliminated, reflecting its low peritoneal clearance. No metabolism or metal transfer of gadodiamine was observed in any patients. …The pharmacokinetic behavior of gadodiamine is consistent with its extracellular distribution. …Studies have shown that gadodiamine is primarily excreted rapidly via the kidneys. In rats, 94% of the administered dose was excreted in the urine within 24 hours of administration. Approximately 1% to 4% of the radioactive material was found in the feces during this period. …In rats, intravenous injection of 14C-labeled gadodiamine (NaCa DTPA-BMA) (0.015 mmol/kg) resulted in a rapid decrease in plasma concentration, with an elimination half-life of 0.31 hours, a volume of distribution of 244 mL/kg, and a plasma clearance of 9.2 mL/min/kg. These results indicate that NaCa DTPA-BMA is distributed in the extracellular fluid and excreted via the kidneys through glomerular filtration. Of the administered radioactive dose, 86.6% was excreted in the urine within 4 hours after injection, 95.3% within 120 hours, and 3.3% in the feces. ...
For more complete data on the absorption, distribution, and excretion of gadodiamines (10 in total), please visit the HSDB record page.

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Metabolism/Metabolites
No biotransformation or degradation of gadodiamines was detected.
Furthermore, experiments were conducted in rats to elucidate the in vivo metabolism of gadodiamines (NaCa DTPA-BMA). Results showed the presence of small amounts of NaCa DTPA-BMA chelates in the urine. High-performance liquid chromatography (HPLC) analysis indicated that these metabolites are zinc (Zn) and copper (Cu) forms of the drug, resulting from the replacement of calcium ions in the NaCa DTPA-BMA molecule by endogenous zinc or copper. Further HPLC and inductively coupled plasma atomic emission spectrometry (ICP-AES) analyses showed that the relative contents of the unchanged parent drug, zinc (Zn), and copper (Cu) forms were approximately 92%, 7%, and 1%, respectively. This indicates that, in vivo, calcium ions in sodium calcium diamine can be replaced by zinc or copper ions, but to a small extent. The mean distribution half-life and elimination half-life (expressed as mean ± standard deviation) were 3.7 ± 2.7 min and 77.8 ± 16 min, respectively. …In rats, after intravenous injection of 14C-labeled gadodiamine (NaCa DTPA-BMA) (0.015 mmol/kg), the plasma concentration of the drug decreased rapidly, with an elimination half-life of 0.31 h… The pharmacokinetic behavior of gadodiamine is consistent with its extracellular distribution. In rats, rabbits, and monkeys, gadodiamine has a short half-life of 18, 38, and 75 minutes, respectively. The pharmacokinetics of intravenously administered gadodiamine in normal subjects conformed to an open two-compartment model, with a mean distribution half-life and elimination half-life (mean ± standard deviation) of 3.7 ± 2.7 minutes and 77.8 ± 16 minutes, respectively. …In 13 patients with abdominal disease undergoing hemodialysis who received intravenous gadodiamine (0.1 mmol/kg body weight), the mean half-life of gadodiamine was 1.93 hours (standard deviation 0.55). Twenty-seven patients were followed up, including nine with severely impaired renal function (glomerular filtration rate 2–10 mL/min), nine on hemodialysis, and nine on continuous ambulatory peritoneal dialysis. Observations were performed at 5, 8, and 22 days after gadodiamine injection (0.1 mmol/kg body weight). Gadolinium injection did not cause changes in renal function. In patients with severely impaired renal function, the elimination half-life of gadodiamine injection (34.3 hours ± 22.9 hours) was prolonged compared to healthy volunteers (1.3 hours ± 0.25 hours).

Toxicity Summary
Identification and Use: Gadolinium is an intravenous contrast agent used in magnetic resonance imaging (MRI) to visualize vascular abnormalities (or lesions believed to cause blood-brain barrier abnormalities) in the brain (intracranial lesions), spine, and related tissues. Human Exposure and Toxicity: The possibility of reactions should always be considered, including serious, life-threatening, fatal anaphylactic or cardiovascular reactions or other specific reactions, especially in patients with a known clinical anaphylaxis, a history of asthma, or other allergic respiratory conditions. Gadolinium contrast agents increase the risk of renal systemic fibrosis (NSF) in patients with acute or chronic severe renal impairment, as well as in patients with any degree of acute renal impairment due to hepatorenal syndrome or perioperative liver transplantation. For these patients, gadolinium contrast agents should be avoided unless diagnostic information is critical and cannot be obtained via non-contrast MRI. Factors that may increase the risk of renal systemic fibrosis (NSF) include repeated use or use of gadolinium contrast agents at doses higher than recommended, and the degree of renal impairment at the time of exposure. Accidental intrathecal administration of Omniscan has occurred, leading to seizures, coma, and sensory and motor dysfunction. In 1157 patients who underwent gadodiamine-enhanced examination, a false decrease in serum calcium levels was observed, from 8.65 mg/dL to 8.33 mg/dL, with 34 patients exhibiting pseudocritical hypocalcemia (<6 mg/dL). In 60 patients with renal insufficiency who received high-dose gadodiamine injections, 36.7% developed pseudocritical hypocalcemia immediately after MRI examination. In 216 patients with renal insufficiency, the mean serum magnesium level slightly increased from 1.69 mEq/L to 1.77 mEq/L after gadodiamine injection. Animal studies: Gadadodiamine injection exhibits extremely low acute lethal toxicity, superior to gadopentetate meglumine or gadoteric acid meglumine injections. Compared to gadopentetate meglumine injection, gadodiamine showed less impact on cardiovascular and hemodynamic function after rapid intravenous administration in anesthetized dogs. Similar to all known intravenous diagnostic imaging agents, gadodiamine injection caused vacuolation of proximal renal tubular cells but did not affect renal function. The degree of vacuolation was moderate and partially subsided within 7 days after administration. Gadodiamine injection did not cause significant irritation when administered via various intravascular and extravascular routes. In monkeys, continuous daily administration of gadodiamine for 28 days had no effect on the kidneys. Monkeys tolerated the compound well, with no adverse reactions observed after 28 days of continuous administration. In rats, significant toxicity was observed only at high doses, particularly in males, and the toxicity pattern (affecting the stomach, testes, and skin) suggested zinc metabolism disorders. Studies in rabbits have shown that gadodiamine at doses up to 5 times the maximum recommended human dose increases the incidence of skeletal and visceral malformations in offspring. Studies have shown that administration of gadodiamine for 13 consecutive days during pregnancy (approximately twice the maximum cumulative dose) can adversely affect embryo-fetal development in rabbits, manifested as an increased incidence of limb flexion and skeletal deformities. Skeletal deformities may be due to maternal toxicity, as the weight of the mother rabbits significantly decreased after gadodiamine administration during pregnancy. The following genotoxicity tests were all negative: bacterial reverse mutation assay, CHO/HGPRT positive mutation assay, CHO chromosomal aberration assay, and in vivo mouse micronucleus assay.

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Effects during pregnancy and lactation
◉ Overview of use during lactation
Gadodiamine releases more free gadolinium than some other gadolinium-containing contrast agents. Some European guidelines recommend suspending breastfeeding for 24 hours after administration, but guidelines developed by several North American professional organizations indicate that breastfeeding women do not need to interrupt breastfeeding after receiving gadolinium-containing contrast agents. Other contrast agents may be more appropriate, especially when breastfeeding newborns or premature infants.
◉ Effects on Breastfed Infants
A mother with neuromyelitis optica was breastfeeding her 38-day-old male infant. Each feeding lasted approximately 15 minutes, every 2 hours. Prior to an MRI scan, she received an injection of gadodiamine (dosage not specified). Breastfeeding was discontinued 6 to 8 hours after the injection. Her infant did not experience any immediate adverse reactions.
◉ Effects on Lactation and Breast Milk
No relevant published information was found as of the revision date.

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Protein Binding
In vitro studies showed that gadodiamine does not bind to human serum proteins.

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Interactions
…In rats receiving weekly intraperitoneal injections of cisplatin (1 mg/kg) for 10 weeks, intravenous injections of saline, iohexol, iohexol, gadopentetate meglumine, and a high dose (4.59 mmol/kg body weight) of gadodiamine were administered, and urinary and serum parameters were monitored for 24 days. Ten rats were in each group. Light and electron microscopy revealed that cisplatin caused severe morphological changes, including renal tubular dilation, atrophy, and necrosis; however, contrast agents did not cause any additional morphological changes. Compared with intravenous saline, gadopentetate dimeglumine, iohexol, and iohexol significantly increased (3-20-fold) proteinuria in the cisplatin nephropathy model, while gadodiamine had no such effect. Proteinuria levels were highest after iohexol injection. All four contrast agents immediately and transiently significantly increased the excretion of brush border enzymes alkaline phosphatase and gamma-glutamyl transferase (125-500-fold) and cytosolic enzymes alanine aminopeptidase and lactate dehydrogenase (16-100-fold). Compared with saline, ionic contrast agents significantly increased glucose (two-fold increase) and sodium (three to five-fold increase) excretion, while non-ionic contrast agents did not have this effect. The authors concluded that high-dose radioactive and magnetic resonance contrast agents cause transient functional impairment in cisplatin-induced nephropathy rats. Gadolinium causes the mildest functional impairment, while iohexol causes the most severe. This article reports a case of a 54-year-old female patient whose serum calcium level was abnormally low after gadodiamine-enhanced magnetic resonance imaging (MRI) using a standard colorimetric method. Two other patients also exhibited the same phenomenon… Repeat serum calcium measurements several hours later were within the normal range. Commercially available gadolinium-based contrast agents may cause abnormally low serum calcium levels when measured using a standard colorimetric method. Physicians' awareness of gadodiamine-induced pseudohypocalcemia may help avoid unnecessary treatment interventions. This article also reports a case of a 78-year-old male patient whose serum calcium level was "extremely low" according to a standard colorimetric method after gadodiamine injection during magnetic resonance angiography. Retesting the same serum sample using absorption spectroscopy showed normal calcium levels, thus confirming a diagnosis of pseudohypocalcemia.

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Non-human toxicity values
Mice intravenous LD50: 14 mmol/kg
Mice intravenous LD50: 34 mmol/kg (gadolinium diamine injection)

[1]. Gadolinium-associated nephrogenic systemic fibrosis: the need for nephrologists' awareness. J Nephrol, 2008. 21(3): p. 324-36.

Gadolinium diamine is a linear, nonionic gadolinium-based contrast agent (GBCA) used in magnetic resonance imaging (MRI) to enhance angiogenesis. GBCAs are the largest class of MRI contrast agents and are generally considered safer than nonionic iodinated contrast agents. Gadolinium diamine was approved by the FDA in 1993 and was the first nonionic GBCA to be put into use. However, because linear nonionic GBCAs are less stable than macrocyclic or ionic GBCAs, gadolinium diamine may lead to increased gadolinium retention in the brain, making it more prone to side effects. Gadolinium diamine is a paramagnetic gadolinium-based contrast agent (GBCA) with imaging activity in magnetic resonance imaging (MRI). When placed in a magnetic field, gadolinium diamine generates a strong local magnetic field, thereby enhancing the relaxation rate of nearby protons. This change in proton relaxation dynamics increases the MRI signal intensity of tissues where gadolinium diamine accumulates; therefore, the imaging of these tissues is enhanced. See also: Gadolinium (note moved to).

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Drug Indications
Gadodiamine is approved by the U.S. Food and Drug Administration (FDA) and Health Canada for the visualization of vascular abnormalities in the brain (intracranial lesions), spine and related tissues, and the body (including the thoracic cavity (non-cardiac), abdominal cavity, pelvic cavity, and retroperitoneal space). Additionally, gadodiamine is approved by Health Canada for the detection and localization of renal artery and aortoiliac artery stenosis in magnetic resonance angiography (MRA).

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Mechanism of Action
Gadodiamine is a paramagnetic molecule that generates a magnetic moment when placed in a magnetic field. This magnetic moment alters the relaxation rate of protons in nearby water within the body. In magnetic resonance imaging (MRI), gadodiamine selectively enhances the contrast of areas of gadodiamine accumulation in tissue.

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Therapeutic Use
Contrast Agent
Omniscan is a gadolinium-based contrast agent for intravenous MRI to visualize lesions with abnormal blood vessels (or those believed to cause blood-brain barrier abnormalities) in the brain (intracranial lesions), spine, and related tissues. /US Product Label Includes/
Omniscan is a gadolinium-based contrast agent for intravenous MRI to aid in visualization of lesions with abnormal blood vessels in the thoracic (non-cardiac), abdominal, pelvic, and retroperitoneal spaces. /US Product Label Includes/
…Evaluating the safety and efficacy of single-dose and triple-dose gadodiamine-enhanced magnetic resonance (MRA) angiography in assessing abdominal arterial stenosis…This randomized, double-blind, phase III, multicenter trial enrolled 105 patients. MRA results at 0.1 mmol/kg and 0.3 mmol/kg doses of gadodiamine were compared with those from digital subtraction angiography (DSA), and patients were grouped according to dose…No serious adverse events were observed. In the proximal region of primary stenosis, the mean contrast index in the three-dose group was significantly higher than that in the single-dose group (P = 0.03). The mean 95% confidence interval for the difference in stenosis severity shown by DSA and enhanced MRA improved from -3.4% ± 4.7 (standard deviation) in the single-dose group to -1.2% ± 4.7 in the three-dose group. Visual analog scale (VAS) showed an improvement in the overall mean image quality in the three-dose group (P = 0.02). The diagnostic confidence of enhanced magnetic resonance angiography (MRA) in the single-dose and triple-dose groups was 88% and 96%, respectively… Both single-dose and triple-dose gadodiamine-enhanced MRA are safe and effective for assessing major abdominal arterial stenosis. Although the concordance between MRA and DSA was high at both doses, triple-dose MRA was superior to single-dose in terms of image quality, degree of arterial stenosis, and diagnostic confidence. ...A double-blind, multicenter, phase III clinical trial evaluated the safety and diagnostic efficacy of MultiHance (gadobacteria meglumine) in the central nervous system (CNS)...The trial recruited 205 patients with a high suspicion of CNS lesions (based on previous imaging findings) at 16 centers in the United States. Patients were randomized to one of three escalating dosing regimens. Magnetic resonance imaging (MRI) was performed using Omniscan (gadobacteria meglumine) at doses of 0.1 and 0.3 mmol/kg, compared with MRI at MultiHance (gadobacteria meglumine) doses of 0.05 and 0.15 mmol/kg and 0.1 and 0.2 mmol/kg...Both the gadolide and gadobacteria groups (single dose and cumulative dose) showed efficacy compared to pre-dose images alone, in terms of diagnostic information level, number of lesions detected, and contrast-to-noise ratio measurements. The diagnostic information level of 0.1 mmol/kg gadobenzamide is comparable to that of gadodiamine at the same dose. One of the two blinded reviewers found that the efficacy of 0.05 mmol/kg gadobenzamide was comparable to that of 0.1 mmol/kg gadodiamine. Both reviewers found that the diagnostic information level was comparable after the second injection of contrast agent in all three dosing regimens. The cumulative dose of gadobenzamide is well tolerated, and its safety profile is comparable to that of gadodiamine… Gadobenzamide is comparable to gadodiamine in safety and efficacy for imaging central nervous system lesions, and may have advantages in imaging applications due to its enhanced T1 relaxation rate.

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Drug Warning
/Black Box Warning/ Warning: Intrathecal administration and use in renal systemic fibrosis (NSF) are contraindicated. Intrathecal administration is contraindicated: Intrathecal administration of OMNISCAN has resulted in seizures, coma, sensory and motor dysfunction. Renal Systemic Fibrosis (NSF): Gadolinium-based contrast agents (GBCAs) increase the risk of NSF in patients with impaired drug clearance. GBCAs should be avoided in these patients unless diagnostic information is critical and cannot be obtained via non-contrast MRI or other examinations. NSF can lead to fatal or disabling fibrosis affecting the skin, muscles, and internal organs. Omniscan is contraindicated in patients with chronic severe kidney disease (glomerular filtration rate (GFR) < 30 mL/min/1.73 m²) or acute kidney injury. Patients should be screened for acute kidney injury and other conditions that may impair kidney function. For patients at risk of chronic kidney decline (e.g., age > 60 years, hypertension, or diabetes), glomerular filtration rate (GFR) should be estimated by laboratory tests. Do not exceed the recommended dose of omesartan and allow sufficient time for the drug to be cleared from the body before re-administering.
Gadolinium-based contrast agents (GBCAs) increase the risk of NSF in patients with impaired drug clearance. GBCA should be avoided in these patients unless diagnostic information is critical and cannot be obtained through non-contrast magnetic resonance imaging (MRI) or other examinations. The risk of GBCA-related NSF appears to be highest in patients with chronic severe kidney disease (glomerular filtration rate (GFR) < 30 mL/min/1.73 m²) and in patients with acute kidney injury. Do not use omesartan in these patients. The risk appears to be lower in patients with chronic moderate kidney disease (GFR 30–59 mL/min/1.73 m²), and very low or no risk in patients with chronic mild kidney disease (GFR 60–89 mL/min/1.73 m²). Renal systemic fibrosis (NSF) can lead to fatal or disabling fibrosis, affecting the skin, muscles, and internal organs. …Screen patients for acute kidney injury and other conditions that may reduce kidney function. Acute kidney injury is characterized by a rapid (within hours to days) and usually reversible decline in kidney function, commonly seen in cases of surgery, severe infection, injury, or drug-induced nephrotoxicity. In cases of acute kidney injury, serum creatinine levels and estimated glomerular filtration rate (eGFR) may not reliably assess renal function. For patients at risk of chronic renal impairment (e.g., age > 60 years, diabetes, or chronic hypertension), eGFR should be estimated by laboratory tests. Factors that may increase the risk of NSF include repeated use or use of gadolinium-based contrast agents (GBCAs) at doses higher than recommended, and the extent of renal impairment at the time of exposure. Record the specific GBCA used by the patient and its dose. When using omesartan, do not exceed the recommended dose and allow sufficient time for complete drug clearance before re-administering. A history of anaphylactic and hypersensitivity reactions with cardiovascular, respiratory, and/or skin manifestations, even leading to death, is present. Before administering omesartan, personnel trained in resuscitation techniques and resuscitation equipment should be present. If a hypersensitivity reaction occurs, immediately stop the omesartan administration and begin appropriate treatment. Patients should be closely monitored during and for several hours after omesartan administration, especially those with a history of drug reactions, asthma, allergies, or other hypersensitivity conditions.
FDA Pregnancy Risk Category: C/Risk cannot be ruled out. There is a lack of adequate, well-controlled human studies, and animal studies have either not shown any risk to the fetus or lack relevant data. There is a possibility of fetal harm if this drug is used during pregnancy. However, the potential benefits may outweigh the potential risks. /
For more complete data on drug warnings for gadodiamine (24 in total), please visit the HSDB record page.

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Pharmacodynamics
In magnetic resonance imaging, the imaging of normal and diseased tissues depends on changes in the intensity of the radiofrequency signal. These changes are due to: variations in proton density; alterations in spin-lattice or longitudinal relaxation time (T1); and variations in spin-spin or transverse relaxation time (T2). Gadadodiamine is a paramagnetic contrast agent whose unpaired electron spins generate a local magnetic field. When water protons pass through this local magnetic field, the change in the magnetic field they experience causes them to redirect to the main magnetic field more quickly than without a paramagnetic contrast agent. By increasing relaxation rate, gadodiamine reduces both T1 and T2 relaxation times in its distributed tissues. At clinical doses, gadodiamine primarily affects T1 relaxation time, leading to increased signal intensity. Blood-brain barrier disruption or vascular abnormalities can cause gadodiamine to accumulate in lesions such as tumors, abscesses, and subacute infarctions. The pharmacokinetic parameters of gadodiamine in various lesions are still unclear.

C16H28GDN5O9

591.6716

592.113

122795-43-1

Gadodiamide;131410-48-5

60754

White to off-white solid powder

769.1ºC at 760mmHg

419ºC

3

12

13

31

527

0

XPCLDSMKWNNKOM-UHFFFAOYSA-K

InChI=1S/C16H29N5O8.Gd.H2O/c1-17-12(22)7-20(10-15(26)27)5-3-19(9-14(24)25)4-6-21(11-16(28)29)8-13(23)18-2;;/h3-11H2,1-2H3,(H,17,22)(H,18,23)(H,24,25)(H,26,27)(H,28,29);;1H2/q;+3;/p-3

2-[bis[2-[carboxylatomethyl-[2-(methylamino)-2-oxoethyl]amino]ethyl]amino]acetate;gadolinium(3+);hydrate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~100 mg/mL (~169.01 mM)
DMSO : ~50 mg/mL (~84.51 mM)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)