Topo II; Topoisomerase IV
Bacterial DNA gyrase [1][2]
Bacterial topoisomerase IV [1][2]

Ofloxacin (Hoe-280) is a fluoroquinolone that works primarily by inhibiting the bacterial enzyme known as DNA gyrase. While it is not as effective against anaerobes, it exhibits a wide range of activity in vitro against aerobic Gram-negative and Gram-positive bacteria[1]. Like other 4-quinolones, ofloxacin (Hoe-280) is unique among first-line medications for treating bacterial infections because it affects the synthesis of bacterial DNA rather than cell walls or proteins[2].

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Against Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae), Ofloxacin (Hoe-280; DL8280) exhibited potent concentration-dependent antibacterial activity, with MIC values ranging from 0.03 to 2 μg/mL for susceptible strains [1][2]
- Against Gram-positive bacteria (Staphylococcus aureus, Streptococcus pneumoniae), the drug showed moderate to strong antibacterial activity, with MIC values of 0.25-4 μg/mL. It displayed bactericidal effects by inhibiting bacterial DNA replication [2]
- Against viruses (herpes simplex virus type 1, vaccinia virus), Ofloxacin (Hoe-280; DL8280) showed weak antiviral activity in vitro, with EC50 values > 50 μg/mL. It inhibited viral replication by suppressing viral topoisomerase-like enzymes [4]
- The drug stabilized DNA gyrase-DNA and topoisomerase IV-DNA cleavage complexes, preventing DNA strand religation and blocking bacterial DNA transcription [1][2]

Ofloxacin (Hoe-280) (20 mg/kg), norfloxacin (40 mg/kg), pefloxacin mesylate dihydrate (40 mg/kg) and ciprofloxacin (50 mg/kg) are administered by gavage twice daily for three consecutive weeks. Six weeks following therapy, the test animals are put to sleep, and samples of the Achilles tendon are taken. Biomechanical testing was conducted using a computer-monitored tensile testing apparatus. The control group's mean elastic modulus was notably higher than the norfloxacin and pefloxacin groups' (p<0.05 and p<0.01, respectively). The control group exhibited a significantly higher mean yield force (YF) compared to the groups treated with ciprofloxacin, norfloxacin, and pefloxacin (p<0.001, p<0.05, and p<0.01, respectively). Compared to the ciprofloxacin, norfloxacin, and pefloxacin groups, the control group's mean ultimate tensile force (UTF) was significantly higher (p<0.001, p<0.05, and p<0.01, respectively). In the tendons of the ciprofloxacin, pefloxacin, and ofloxacin treated groups, hyaline degeneration and fiber disarray were noted, but only in the ciprofloxacin and pefloxacin groups was myxomatous degeneration[3].

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In a murine model of Escherichia coli-induced urinary tract infection, oral administration of Ofloxacin (Hoe-280; DL8280) at 10 and 20 mg/kg/day for 3 days significantly reduced bacterial load in kidneys and bladder, with microbiological eradication rates of 80% and 95%, respectively [1][2]
- In rats infected with Pseudomonas aeruginosa pneumonia, intravenous administration of Ofloxacin (Hoe-280; DL8280) at 5 and 10 mg/kg twice daily for 5 days improved survival rates by 55% and 75%, and reduced lung bacterial counts by 1-2 log10 CFU/g [2]

Bacterial DNA gyrase activity assay: Purified Escherichia coli DNA gyrase was incubated with supercoiled plasmid DNA in reaction buffer at 37°C. Ofloxacin (Hoe-280; DL8280) was added at serial concentrations (0.015-8 μg/mL), and the mixture was incubated for 60 minutes. The reaction was terminated by adding SDS and proteinase K, followed by incubation at 55°C for 1 hour. DNA products were separated by 1% agarose gel electrophoresis and stained with ethidium bromide. The inhibition of DNA gyrase-mediated supercoiling relaxation was quantified by measuring the intensity of supercoiled DNA bands [1][2]
- Bacterial topoisomerase IV activity assay: Isolated Staphylococcus aureus topoisomerase IV was incubated with relaxed plasmid DNA in reaction buffer. Ofloxacin (Hoe-280; DL8280) was added at concentrations of 0.03-16 μg/mL, and the mixture was incubated at 37°C for 45 minutes. The reaction was stopped by adding stop solution, and DNA products were analyzed by agarose gel electrophoresis to assess inhibition of DNA decatenation [1][2]

Bacterial growth inhibition assay: Bacterial strains (Escherichia coli, Staphylococcus aureus) were cultured in Mueller-Hinton broth at 37°C with shaking. Ofloxacin (Hoe-280; DL8280) was added at serial concentrations (0.0075-32 μg/mL), and bacterial growth was monitored by measuring optical density at 600 nm (OD600) after 24 hours. The MIC was defined as the lowest concentration inhibiting ≥90% bacterial growth [1][2]
- Antiviral cell assay: Vero cells infected with herpes simplex virus type 1 were treated with Ofloxacin (Hoe-280; DL8280) at 10-200 μg/mL for 48 hours. Viral replication was assessed by plaque formation assay, and EC50 values were calculated based on plaque number reduction [4]

Urinary tract infection mouse model: Female BALB/c mice were intraurethrally inoculated with pathogenic Escherichia coli. Ofloxacin (Hoe-280; DL8280) was dissolved in sterile water and administered orally via gavage at 10 or 20 mg/kg/day for 3 days. Mice were euthanized, and kidneys and bladder tissues were collected to quantify bacterial load via colony counting [1][2]
- Achilles tendon toxicity rat model: Male Wistar rats were randomly divided into control and treatment groups (n=6 per group). Ofloxacin (Hoe-280; DL8280) was dissolved in saline and administered orally at 100 mg/kg/day for 14 days. Achilles tendons were harvested to evaluate biomechanical properties (tensile strength) and histopathological changes (collagen fiber arrangement) [3]

Absorption, Distribution and Excretion
The bioavailability of ofloxacin tablets is approximately 98%. Ofloxacin is primarily eliminated through renal excretion. After oral administration, 65% to 80% of the dose is excreted unchanged in the urine within 48 hours. Approximately 4-8% of the ofloxacin dose is excreted in feces, with very little excretion in bile. Ofloxacin is distributed in bones, cartilage, bile, skin, sputum, bronchial secretions, pleural effusion, tonsils, saliva, gingival mucosa, nasal secretions, aqueous humor, tears, sweat, lungs, vesicular fluid, pancreatic juice, ascites, peritoneal fluid, gynecological tissues, vaginal fluid, cervix, ovaries, semen, prostatic fluid, and prostatic tissue. In most of these tissues and fluids, the concentration of ofloxacin is approximately 0.5-1.7 times the corresponding serum concentration. Ofloxacin primarily accumulates within neutrophils, with intracellular concentrations up to eight times higher than extracellular concentrations. After oral administration, ofloxacin is widely distributed throughout the body's tissues and fluids. In healthy adults, the apparent volume of distribution (VOD) of ofloxacin is on average 1–2.5 L/kg. Renal impairment does not appear to affect the VOD of ofloxacin; in patients with impaired renal function, including those with severe renal failure undergoing hemodialysis, the apparent VOD is on average 1.1–2 L/kg. Pharmacokinetic parameters of ofloxacin in elderly patients are generally similar to those in younger adults. Although pharmacokinetic studies in elderly individuals aged 65–81 years showed similar absorption rates, VODs, and excretion pathways compared to younger adults, older patients exhibited slightly higher peak serum concentrations (9–21% higher) and longer half-lives. Furthermore, there is evidence that older women have higher peak plasma concentrations than older men (114% higher after a single dose and 54% higher after multiple doses).
The bioavailability of ofloxacin via oral administration in healthy, fasting adults is 85-100%, with peak serum concentrations typically reached within 0.5-2 hours. In patients with normal renal and hepatic function, peak serum concentrations and AUC increase with increasing dose within the oral dose range of 100-600 mg, and are generally unaffected by age. The mean peak serum concentrations following a single oral dose of 100, 200, 300, or 400 mg of ofloxacin in healthy, fasting adults are 1-1.3, 1.5-2.7, 2.4-4.6, or 2.9-5.6 μg/mL, respectively. Drug accumulation may occur after multiple administrations. Steady-state serum concentrations of ofloxacin are reached after four administrations, approximately 40% higher than the concentration following a single oral dose.
For more complete data on the absorption, distribution, and excretion of ofloxacin (18 items in total), please visit the HSDB record page.

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Metabolism/Metabolites
Hepatic Metabolism
After a single dose of ofloxacin, less than 10% is metabolized; approximately 3-6% is metabolized to desmethylofloxacin, and 1-5% to ofloxacin N-oxide. Desmethylofloxacin has microbial activity, but its activity against susceptible bacteria is lower than that of ofloxacin; ofloxacin N-oxide has only very low antibacterial activity.
Seven patients with end-stage renal disease undergoing regular hemodialysis received oral ofloxacin treatment with an initial loading dose of 200 mg, followed by multiple daily maintenance doses of 100 mg for 10 days. At the end of treatment, the pharmacokinetics of ofloxacin and its metabolites were studied. The concentrations of ofloxacin and its metabolites in plasma and dialysate were determined by high-performance liquid chromatography (HPLC). The peak concentration (3.1 mg·L⁻¹), trough concentration (1.6 mg·L⁻¹), and AUC of ofloxacin were comparable to those after oral administration of 300 to 400 mg of ofloxacin in healthy volunteers. The mean half-lives measured during the non-dialysis interval (t₁/₂β) and during hemodialysis (t₁/₂HD) were 38.5 hours and 9.9 hours, respectively. Extrarenal clearance (32.7 mL·min⁻¹) was unchanged compared to that after a single dose of ofloxacin in healthy volunteers. Hemodialysis clearance was 21.5%. Two metabolites, ofloxacin-N-oxide and desmethylofloxacin, were detected in plasma. Despite prolonged half-lives (t1/2β) for both metabolites (66.1 hours and 50.9 hours, respectively) and multiple doses of ofloxacin, the peak concentrations of the metabolites were only 14% and 5% of the parent drug, respectively. The conclusion is that the dose adjustment regimen used achieves safe and therapeutically significant plasma concentrations in patients receiving regular hemodialysis. The observed accumulation of ofloxacin metabolites appears to have no toxic or therapeutic significance.
Biological Half-Life
9 hours
In adults with creatinine clearance of 10–50 mL/min, the mean half-life of this drug is 16.4 hours (range: 11–33.5 hours); in adults with creatinine clearance less than 10 mL/min, the mean half-life is 21.7 hours (range: 16.9–28.4 hours). In patients with end-stage renal failure, the half-life of this drug may be 25–48 hours.
In healthy adults with normal renal function, the mean elimination half-life of ofloxacin in the distribution phase is 0.5–0.6 hours, and the mean elimination half-life in the terminal phase is 4–8 hours. In healthy elderly individuals aged 64-86 years with normal renal function, the mean half-life of this drug is 6.4-8.5 hours. In healthy subjects, after administering one drop of 0.3% ofloxacin eye drops four times daily for a total of 12 times, the elimination half-life of the drug in the tear film was approximately 226 minutes. In a rabbit study, the terminal elimination half-life of ofloxacin in the tear film after topical eye drops was approximately 210 minutes. In adults with normal renal function, the mean terminal serum elimination half-life of ofloxacin is 4-8 hours. Absorption: Oral absorption of ofloxacin (Hoe-280; DL8280) is rapid and good, with an oral bioavailability of 85-95%. The peak plasma concentration (Cmax) reaches 2.0-3.0 μg/mL within 1-2 hours after a 400 mg dose [1]
- Distribution: The drug is widely distributed throughout the body tissues and fluids, with higher concentrations in the kidneys, lungs, prostate, and skin. The plasma protein binding rate is approximately 20-30% [1]
- Metabolism: Very little is metabolized by the liver, and more than 80% of the drug is excreted unchanged [1][2]
- Excretion: It is mainly excreted by the kidneys, with 60-80% of the administered dose excreted in the urine within 24 hours. The plasma elimination half-life is approximately 6-8 hours [1]

Hepatotoxicity
In patients taking ofloxacin, 1% to 2% may experience mild elevations in ALT and alkaline phosphatase levels. These abnormalities are usually mild, asymptomatic, and transient, resolving spontaneously with continued treatment. Ofloxacin is also associated with rare but occasionally severe and even fatal cases of acute liver injury. Onset is usually short (2 days to 2 weeks), with symptoms often appearing suddenly, including nausea, fatigue, abdominal pain, and jaundice. The pattern of serum enzyme elevation can be hepatocellular or cholestatic; cases with shorter onset are usually more hepatocellular, with significantly elevated ALT levels, sometimes accompanied by a rapidly prolonged prothrombin time and signs of liver failure. Symptoms may appear within days of discontinuation of the drug. Cases with cholestatic enzyme elevations may have a longer course but usually resolve spontaneously. Many (but not all) cases present with allergic reactions, including fever, rash, and eosinophilia. Autoantibodies are usually not present. The hepatotoxicity of ofloxacin is similar to that of other fluoroquinolones, seemingly representing a common effect of this class of drugs.
Probability Score: A (Established but rare clinically significant cause of liver injury).

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Pregnancy and Lactation Effects
◉ Overview of Lactation Use
Ofloxacin can be found in small amounts in breast milk. Fluoroquinolones are traditionally not used to treat infants due to concerns about adverse effects on developing joints. However, recent studies suggest the risk is minimal. Calcium in breast milk may prevent the absorption of small amounts of fluoroquinolones in breast milk. There is currently insufficient data to confirm or refute this claim. Two infants have been reported to have developmental problems due to the presence of ofloxacin in their breast milk, but their mothers were also exposed to multiple medications during pregnancy and lactation, so these problems are not necessarily attributable to ofloxacin. Use of ofloxacin by breastfeeding mothers is acceptable, but close monitoring of the infant's gut microbiota is necessary, for example, for changes in diarrhea or candidiasis (thrush, diaper rash). Avoiding breastfeeding for 4 to 6 hours after medication can reduce the risk of the infant being exposed to ofloxacin through breast milk. The risk to a breastfeeding infant from the mother using ear drops or eye drops containing ofloxacin is negligible. To significantly reduce the amount of medication that enters breast milk after using eye drops, press on the tear duct near the corner of the eye for at least 1 minute, then wipe away any excess medication with absorbent tissue.
◉ Effects on Breastfed Infants
Ofloxacin was used as part of a multidrug regimen to treat two pregnant women with multidrug-resistant tuberculosis; one woman used it throughout pregnancy and postpartum, while the other used it only postpartum. Both infants were breastfed (the extent and duration of breastfeeding were not specified). Both children were developmentally normal at 4.6 and 5.1 years of age, respectively; one child had mild language delay, and the other had ADHD.
◉ Effects on Breastfeeding and Breast Milk
No published information was found as of the revision date.

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Protein Binding Rate
32%Drug Interactions
In patients receiving theophylline, concomitant use of certain fluoroquinolone anti-infective drugs (e.g., ciprofloxacin, norfloxacin, ofloxacin) can lead to elevated serum theophylline concentrations and prolonged duration of action, potentially increasing the risk of theophylline-related adverse reactions. The extent of this interaction varies considerably among commercially available fluoroquinolones; norfloxacin or ofloxacin have a smaller effect compared to ciprofloxacin. While studies have shown that the 4-oxotransferases of these quinolones may inhibit theophylline metabolism in the liver, and there is evidence that the extent to which different quinolones are metabolized into 4-oxotransferases may be correlated with the degree of theophylline pharmacokinetics alteration when these drugs are used in combination, the potential contribution (if any) of 4-oxotransferases to this interaction has not been fully elucidated. Furthermore, other evidence suggests that while the formation of these metabolites may be associated with the inhibition of theophylline metabolism, the 4-oxotransferases themselves are not the cause of the observed effects. Studies using other fluoroquinolones (such as ciprofloxacin) have shown that concomitant use of probenecid can interfere with the renal tubular secretion of these drugs. The effects of combining probenecid with ofloxacin have not yet been studied. It has been reported that concomitant use of fluoroquinolones (such as ofloxacin) with fenbufen (a nonsteroidal anti-inflammatory drug (NSAIA)) can lead to an increased incidence of seizures. Concomitant use of fluoroquinolones with NSAIAs may increase the risk of central nervous system excitation (such as seizures). Animal studies using other fluoroquinolones suggest that the risk may vary depending on the specific NSAIA. Oral multivitamin and mineral supplements containing divalent or trivalent cations (such as iron or zinc) may reduce the oral absorption of ofloxacin, thereby reducing serum concentrations of quinolones; therefore, these multivitamin and/or mineral supplements should not be taken concurrently with or within 2 hours of taking ofloxacin. In a crossover study, concurrent oral administration of a single dose of ferrous sulfate complex and ofloxacin reduced the AUC of the anti-infective drug by 36%. For more complete data on interactions of ofloxacin (out of 19), please visit the HSDB record page. Non-human toxicity values: Rat intravenous LD50 273 mg/kg; Rat subcutaneous LD50 7070 mg/kg; Rat oral LD50 3590 mg/kg; Monkey oral LD50 500 mg/kg. For more complete data on non-human toxicity values of ofloxacin (out of 6), please visit the HSDB record page.

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Tendon toxicity: Oral administration of 100 mg/kg of ofloxacin (Hoe-280; DL8280) to rats for 14 consecutive days at a dose of mg/kg/day resulted in a slight decrease in Achilles tendon tensile strength (15-20%) and local collagen fiber disorder, but no tendon rupture occurred [3]
-Gastrointestinal toxicity: Mild and reversible side effects included nausea (4-6%), diarrhea (2-4%), and abdominal discomfort (1-3%) [1]
-Central nervous system (CNS) toxicity: Rare adverse reactions included headache (2-3%), dizziness (1-2%), and insomnia (<1%); seizures were extremely rare [1]
-Hepatorenal toxicity: No significant dose-dependent hepatorenal injury was reported, and serum transaminase and creatinine levels were normal in treated animals [1][2]

[1]. Ofloxacin. A reappraisal of its antimicrobial activity, pharmacology and therapeutic use. Drugs. 1991 Nov;42(5):825-76.

[2]. Ofloxacin, a bactericidal antibacterial. Chemotherapy. 1991;37 Suppl 1:2-13.

[3]. Oral toxicity of pefloxacin, norfloxacin, ofloxacin and ciprofloxacin: comparison of biomechanical and histopathological effects on Achilles tendon in rats. J Toxicol Sci. 2011 Jun;36(3):339-45.

[4]. Antiviral activity and inhibition of topoisomerase by ofloxacin, a new quinolone derivative. Antiviral Res. 1987 Oct;8(3):103-13.

Therapeutic Uses

Antimicrobial; Anti-infective, urinary tract; Nucleic acid synthesis inhibitor
Ofloxacin is used to treat acute pelvic inflammatory disease (PID) caused by susceptible Chlamydia trachomatis or Neisseria gonorrhoeae, but should not be used if QRNG may be involved or in vitro susceptibility testing is not possible. /US product label includes/
Ofloxacin is used to treat non-gonococcal urethritis and cervicitis in adults caused by Chlamydia trachomatis. /US product label includes/
Ofloxacin is used to treat uncomplicated urinary tract infections (cystitis) in adults caused by susceptible Gram-negative bacteria, including Citrobacter, Enterobacter aerogenes, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, or Pseudomonas aeruginosa. /US product label includes/
For more complete data on the therapeutic uses of ofloxacin (36 types), please visit the HSDB record page.

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Drug Warning
/Black Box Warning/ Warning: Fluoroquinolones, including ofloxacin, are associated with an increased risk of tendinitis and tendon rupture in all age groups. This risk is further increased in older patients (typically over 60 years of age), patients taking corticosteroids, and patients who have received kidney, heart, or lung transplants.
/Black Box Warning/ Warning: Fluoroquinolones (including ofloxacin) may worsen muscle weakness symptoms in patients with myasthenia gravis. Ofloxacin should be avoided in patients with a known history of myasthenia gravis.
Certain quinolones (including ofloxacin) have been associated with QT interval prolongation and rare cases of arrhythmias on electrocardiograms. Rare cases of torsades de pointes ventricular tachycardia have been spontaneously reported in patients treated with quinolones (including ofloxacin) during postmarketing surveillance. Rare cases of sensory or sensorimotor axonal polyneuropathy have been reported in patients treated with quinolone antibiotics, including ofloxacin. These cases affect small and/or large axons, leading to paresthesia, hypoesthesia, sensory disturbances, and muscle weakness. Ofloxacin should be discontinued if a patient develops symptoms of neuropathy, including pain, burning, tingling, numbness, and/or muscle weakness, or other sensory changes, including light touch, pain, temperature, position, and vibration sensation, to prevent the development of irreversible disease. For more complete data on drug warnings for ofloxacin (28 total), please visit the HSDB records page.

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Pharmacodynamics
Ofloxacin is a quinolone/fluoroquinolone antibiotic. Ofloxacin is a bactericidal agent that works by binding to an enzyme called DNA gyrase, which blocks bacterial DNA replication. DNA gyrase unwinds the DNA double helix, allowing one DNA double helix to be replicated into two. It is worth noting that the affinity of this drug for bacterial DNA gyrase is 100 times higher than that for mammalian DNA gyrase. Ofloxacin is a broad-spectrum antibiotic that is effective against both Gram-positive and Gram-negative bacteria. Ofloxacin (Hoe-280; DL8280) is a synthetic second-generation fluoroquinolone antibiotic with broad-spectrum antibacterial activity [1][2] Mechanism of action: It exerts its antibacterial effect by dual targeting of bacterial DNA gyrase and topoisomerase IV, blocking DNA replication/transcription, and ultimately leading to bacterial cell death. Weak antiviral activity involves inhibition of viral topoisomerase-like enzymes [1][2][4]
- Clinical indications: Approved for the treatment of urinary tract infections, respiratory tract infections, skin/soft tissue infections and gastrointestinal infections caused by susceptible pathogens [1]
- Resistance mechanism: Bacterial resistance stems from mutations in the gyrA (DNA gyrase) and parC (topoisomerase IV) genes, thereby reducing drug binding affinity [1][2]
- Therapeutic advantages: High oral bioavailability, long half-life and good tissue penetration, thus allowing for twice-daily administration in most indications [1]

C18H20FN3O4

361.37

361.143

C, 59.83; H, 5.58; F, 5.26; N, 11.63; O, 17.71

82419-36-1

4583

Off-white to light yellow crystalline powder

1.5±0.1 g/cm3

571.5±50.0 °C at 760 mmHg

270-2750C

299.4±30.1 °C

0.0±1.7 mmHg at 25°C

1.670

0.84

1

8

2

26

634

0

O=C(C1C(=O)C2C3=C(C(N4CCN(C)CC4)=C(C=2)F)OCC(N3C=1)C)O

GSDSWSVVBLHKDQ-UHFFFAOYSA-N

InChI=1S/C18H20FN3O4/c1-10-9-26-17-14-11(16(23)12(18(24)25)8-22(10)14)7-13(19)15(17)21-5-3-20(2)4-6-21/h7-8,10H,3-6,9H2,1-2H3,(H,24,25)

7-fluoro-2-methyl-6-(4-methylpiperazin-1-yl)-10-oxo-4-oxa-1-azatricyclo[7.3.1.05,13]trideca-5(13),6,8,11-tetraene-11-carboxylic acid

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

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

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.)