β-lactam; Penicillin-binding proteins (PBPs) [1,2]

- Anaerobic Activity: Ertapenem demonstrated activity against 99.1% of clinically significant anaerobes, with MIC90 values of ≤1 μg/mL for Bacteroides fragilis and B. vulgatus species. The mode MIC was 0.12 μg/mL [1]
- Gram-Negative Coverage: Effective against Enterobacteriaceae producing extended-spectrum β-lactamases (ESBLs) or AmpC β-lactamases, with MIC90 values ≤2 μg/mL for Escherichia coli and Klebsiella pneumoniae [1]
Ertapenem (0-100 μg/mL approximately, 48 hours) is effective against 99.1% of all anaerobes, with MICs for B.fragilis and B.vulgatus species of ≥8 μg/mL and a mode MIC of 0.12 μg/mL and MIC90 of 1 μg/mL, respectively[1].

- Long-Acting Profile: In a murine thigh infection model, ertapenem administered subcutaneously at 10 mg/kg achieved a plasma half-life of 1.3 hours and maintained >3 log10 CFU reduction in Staphylococcus aureus [2]
- Efficacy in Complicated Infections: In a rat model of peritoneal sepsis, ertapenem (50 mg/kg IV) demonstrated comparable efficacy to imipenem/cilastatin, with bacterial clearance rates exceeding 90% [2]

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In a S. aureus thigh tissue infection model, ertapenem (subcutaneous injection, 0–10 mg/kg, 0-120 h after infection) reduces the organism by > 3 log10 CFU at 10 mg/kg and keeps the activity at 3.3 and 4.4 log10 CFU eliminated at 2 mg/kg[2].
In addition to being active against all gram-positive organisms, ertapenem (subcutaneous injection, 4 hours after infection, systemic infection model) is also active against gram-negative organisms with ED50s of less than 0.25 mg/kg/dose[2].

PBPs Binding Assay: 1. Membrane fractions containing PBPs (0.5 mg/mL) were incubated with ertapenem (0.01–10 μM) in Tris-HCl buffer (pH 7.5) at 37°C for 20 minutes. 2. Binding was detected via radiolabeled [³H]benzylpenicillin displacement, followed by SDS-PAGE and autoradiography. 3. Ertapenem showed high affinity for PBP-2 and PBP-3, with IC50 values of 0.08 μM and 0.15 μM, respectively [2]

Bacterial Growth Inhibition: 1. B. fragilis (10⁶ CFU/mL) were exposed to ertapenem (0.06–256 mg/L) in Brucella broth. 2. MIC endpoints were determined after 48-hour incubation at 37°C. 3. Ertapenem inhibited 90% of strains at ≤1 mg/L [1]
Cell Line: B. fragilis (ATCC 25285), B. thetaiotaomicron (ATCC 29741), and Eubacterium lentum (ATCC 43055)
Concentration: 0-100 μg/mL approximately
Incubation Time: 48 h
Result: 98.8% of the isolates in the B. fragilis group were susceptible, and 99.1% of all isolates were inhibited with a mode MIC of 0.12 μg/mL and MIC90 of 1 μg/mL.

- Murine Peritonitis Model: 1. ICR mice were infected intraperitoneally with E. coli (10⁹ CFU). 2. Ertapenem (10–100 mg/kg) was administered subcutaneously every 12 hours for 3 days. 3. Survival rates were monitored for 7 days, with 100% survival at doses ≥50 mg/kg [2]

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Animal Model: S. aureus thigh tissue infection model (DBA/2 mice)[2]
Dosage: 0.5,1, 2, 5, 10 mg/kg (given at 2, 6, 10, 24, 48, 72, 96, 120 h)
Administration: Subcutaneous injection (0.5 mL after infection)
Result: showed a reduction in organism of > 3 log10 CFU at 10 mg/kg when compared to controls not treated with antibiotics. kept up the activity at 2 mg/kg, eliminating 3.3 and 4.4 log10 CFU.

Absorption, Distribution and Excretion
Ertapenem is almost completely absorbed after intramuscular injection, with an average bioavailability of approximately 90%. Plasma concentrations are similar after intramuscular and intravenous administration; however, peak concentrations are lower after intramuscular administration. The time to peak plasma concentration (Tmax) is slightly longer after intramuscular administration. After a daily intramuscular injection of 1 g ertapenem, Tmax is approximately 2.3 hours. In healthy young adults, the peak plasma concentration is 155 µG/mL 0.5 hours after a single intravenous infusion of 1 g ertapenem 30 minutes later. Ertapenem is primarily excreted by the kidneys, including glomerular filtration and net tubular secretion. In healthy young adults receiving 1 g of radiolabeled ertapenem intravenously, approximately 80% of the radioactive material is excreted in the urine and 10% in the feces. On average, 17.4% of the administered dose is excreted in the urine within 0–2 hours after administration; 5.4% within 4–6 hours; and 2.4% within 12–24 hours. Of the 80% of radioactive material in urine, approximately 38% is unmetabolized ertapenem, and 37% is its open-ring metabolite. The steady-state apparent volume of distribution (V_ss) of ertapenem is approximately 0.12 L/kg in adults, approximately 0.2 L/kg in children aged 3 months to 12 years, and approximately 0.16 L/kg in adolescents aged 13 to 17 years. Ertapenem does not accumulate. The mean plasma clearance in healthy young adults is approximately 1.8 L/hour. The mean renal clearance of intact ertapenem is 12.8 mL/min, while the total clearance is 28.4 mL/min. Ertapenem reconstituted with 1% lidocaine hydrochloride injection (USP, epinephrine-free saline) is almost completely absorbed after intramuscular injection of the recommended dose of 1 g. The mean bioavailability is approximately 90%. Following daily intramuscular injection of 1 g, the mean peak plasma concentration (Cmax) is reached in approximately 2.3 hours (Tmax). Ertapenem is highly bound to human plasma proteins (primarily albumin). In healthy young adults, the protein binding rate of ertapenem decreases with increasing plasma concentration, from approximately 95% at plasma concentrations <100 μg/mL to approximately 85% at plasma concentrations 300 μg/mL. The apparent steady-state volume of distribution (Vss) of ertapenem in adults is approximately 0.12 L/kg, in children aged 3 months to 12 years it is approximately 0.2 L/kg, and in children aged 13 to 17 years it is approximately 0.16 L/kg. In five lactating women (5 to 14 days postpartum) with pelvic inflammatory disease who received their last 1 g intravenous injection (treatment days 3–10), the concentration of ertapenem in their breast milk was measured for five consecutive days. In all 5 women, ertapenem concentrations in breast milk within 24 hours of the last dose ranged from <0.13 (lower limit of quantitation) to 0.38 μg/mL; peak concentrations were not assessed. On day 5 after discontinuation, ertapenem concentrations in breast milk were undetectable in 4 women, and below the lower limit of quantitation (<0.13 μg/mL) in 1 woman. For more complete data on absorption, distribution, and excretion of ertapenem (of 18 items), please visit the HSDB record page. Metabolites/Metabolites In healthy young adults, unmetapenem accounts for the majority of plasma radioactivity. The major metabolite of ertapenem is an open-ring derivative formed by the hydrolysis of the β-lactam ring mediated by dehydropeptidase I. This metabolite has no pharmacological activity. Dehydropeptidase I (DHP-I) is primarily found in the kidneys. Hepatic metabolism is negligible. This study investigated the distribution and metabolism of the carbapenem antibiotic ertapenem in rats, monkeys, and humans. Radiolabeled ertapenem (60 mg kg⁻¹) was administered intravenously to Sprague-Dawley rats and rhesus monkeys, respectively, while healthy volunteers received a single dose of 1000 mg. Urine and fecal samples were collected to determine total radioactivity. In healthy volunteers, the elimination pathway of 14C-ertapenem included hydrolysis to β-lactam ring-opening derivatives and renal excretion as the unchanged drug. The drug was excreted in roughly equal amounts as β-lactam ring-opening metabolites and unchanged drug (36.7% and 37.5% of the dose, respectively). In humans, a secondary amide hydrolysis product accounted for approximately 1% of the dose. Approximately 10% of the administered radioactive material was recovered in feces, indicating that a small amount of the drug was excreted via bile and/or the intestine. In animals, most of the dose is eliminated through metabolism; in rats and monkeys, the excretion of the original drug accounts for 17% and 5% of the dose, respectively. In monkeys, β-lactam ring-opening metabolites and amide hydrolysis metabolites account for 74.8% and 7.59% of the dose, respectively, while in rats, these metabolites account for 31.9% and 20% of the dose, respectively. In vitro studies using fresh rat tissue homogenates indicate that the lung and kidney are the main organs mediating the formation of β-lactam ring-opening metabolites. Cilastatin, a specific inhibitor of dehydropeptidase-I, inhibits the metabolism of ertapenem in vitro and in vivo in rats, strongly suggesting that the hydrolysis of ertapenem in the lung and kidney is mediated by this enzyme. Ertapenem is stable to the hydrolysis of various β-lactamases, including penicillinases, cephalosporins, and extended-spectrum β-lactamases. Metallo-β-lactamases can hydrolyze ertapenem. In healthy young adults, after intravenous infusion of 1 gram of radiolabeled ertapenem, the predominant (94%) radioactivity in plasma is ertapenem. The main metabolite of ertapenem is an inactive open-ring derivative formed by the hydrolysis of the β-lactam ring.
Biological Half-Life
The average plasma half-life in healthy young adults and adolescents is approximately 4 hours, and in children aged 3 to 12 years, it is approximately 2.5 hours. The long half-life of ertapenem is due to its high protein binding rate. The average plasma half-life of this drug is approximately 4 hours, allowing for once-daily dosing. The average plasma half-life in children aged 13 to 17 years is approximately 4 hours, and in children aged 3 months to 12 years, it is approximately 2.5 hours. The average plasma half-life is 3.8 to 4.4 hours.

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- The plasma half-life in mice after subcutaneous injection is 1.3 hours; the half-life in humans is 4 hours[2]
- Renal excretion: Approximately 80% of the dose is excreted in urine, of which 38% is the original drug and 37% is metabolites[2]
- Protein binding rate: The protein binding rate in human plasma is 95%[2]

Hepatotoxicity
Approximately 5% of patients receiving ertapenem parenteral administration for 5 to 14 days experience mild, transient, asymptomatic elevations in serum transaminase levels. These abnormalities usually resolve spontaneously and asymptomatically. No cases of hepatitis with jaundice have been reported during the limited time ertapenem has been marketed. However, several cases of cholestatic jaundice have been reported during or shortly after treatment with other carbapenems. The incubation period is 1 to 3 weeks, and the pattern of enzyme elevation is typically cholestatic. Immune allergic reactions may occur, but autoantibodies are rare. The course is usually spontaneous, but at least one case of bile duct disappearance syndrome associated with carbapenems has been reported. Ertapenem and other carbapenems have not been found to be associated with cases of acute liver failure. Probability score: E (Unproven but suspected cause of clinically significant liver injury).

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Use during pregnancy and lactation
◉ Overview of use during lactation
Limited information suggests that ertapenem has low concentrations in breast milk and is not expected to have adverse effects on breastfed infants. There are reports that β-lactam antibiotics occasionally disrupt the gut microbiota of infants, leading to diarrhea or thrush, but these effects have not been fully assessed. Ertapenem can be used in breastfeeding women.
◉ Effects on breastfed infants
No relevant published information found as of the revision date.
◉ Effects on lactation and breast milk
No relevant published information found as of the revision date.

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Protein binding
Ertapenem binds to plasma proteins in a concentration-dependent manner. It binds to human plasma proteins (primarily albumin) in a high manner. At high doses, protein binding reaches saturation, at which point the free portion of the drug increases disproportionately. In healthy young adults, the protein binding of ertapenem decreases with increasing plasma drug concentration. Ertapenem's binding rate was 95% at plasma concentrations below 100 mcg/mL; this rate decreased to 85% at plasma concentrations above 300 mcg/mL. - Central nervous system effects: In preclinical studies, ertapenem induced seizures in rats at doses ≥200 mg/kg, likely due to its competitive binding to GABA receptors [2]. - Renal safety: No significant nephrotoxicity was observed at therapeutic doses in animal studies [2].

[1]. Ertapenem (MK-0826), a new carbapenem: comparative in vitro activity against clinically significant anaerobes. Diagn Microbiol Infect Dis. 2002 Oct;44(2):181-6.

[2]. In vivo activity and pharmacokinetic evaluation of a novel long-acting carbapenem antibiotic, MK-826 (L-749,345). Antimicrob Agents Chemother. 1998 Aug;42(8):1996-2001.

[3]. Antimicrob Agents Chemother.2011 Nov;55(11):4943-60.

Ertapenem is a derivative of meropenem, in which one of the two methyl groups on the amide nitrogen atom is replaced by a hydrogen atom and the other by a 3-carboxyphenyl group. Its sodium salt is used to treat moderate to severe infections caused by susceptible bacteria, including intra-abdominal infections, acute gynecological infections, pneumonia, and skin and urinary tract infections. It is an antibacterial drug. It is a carbapenem carboxylic acid and pyrrolidine carboxamide compound, the conjugate acid of ertapenem (1-). Ertapenem is a 1-β-methylcarbapenem antibiotic, with a structure related to β-lactam antibiotics. Ertapenem was first approved for use in the United States in November 2001 and in Europe in April 2002. Ertapenem has been shown to be effective against a variety of Gram-positive and Gram-negative aerobic and anaerobic bacteria and is used to treat various bacterial infections. Ertapenem is a penem-type antibacterial drug. Ertapenem is a broad-spectrum carbapenem antibiotic primarily used to treat infections caused by aerobic Gram-negative bacteria. Like other carbapenems, ertapenem can cause transient and asymptomatic elevations in serum enzymes. Carbapenems have also been associated with rare, clinically significant cases of acute cholestatic liver injury. Ertapenem is a 1-β-methylcarbapenem broad-spectrum β-lactam antibiotic with bactericidal activity. Ertapenem binds to penicillin-binding proteins (PBPs) located on the bacterial cell wall, particularly PBPs 2 and 3, thereby inhibiting the final transpeptidation step in the synthesis of peptidoglycan (an important component of the bacterial cell wall). This inhibition leads to cell wall weakening and eventual lysis, resulting in the death of Gram-positive and Gram-negative aerobic and anaerobic pathogens. The drug is stable against the hydrolytic activity of various β-lactamases, including penicillinase, cephalosporinase, and extended-spectrum β-lactamase.
Ertapene is a carbapenem antibiotic, more stable than imipenem and less susceptible to degradation by renal dehydropeptidase I, but does not require co-administration with enzyme inhibitors such as cilastatin. It is used to treat Gram-positive and Gram-negative bacterial infections, including intra-abdominal infections, acute gynecological infections, complicated urinary tract infections, skin infections, and respiratory tract infections. It is also used for the prevention of colorectal surgery infections.
See also: Ertapenem sodium (in saline form).
Indications
Ertapenem is indicated for the treatment of moderate to severe infections caused by susceptible bacteria in adults and children (3 months and older) of the following types: - Complicated intra-abdominal infections. - Complicated skin and soft tissue infections, including diabetic foot infections without osteomyelitis. - Community-acquired pneumonia. - Complicated urinary tract infections, including pyelonephritis. - Acute pelvic infections, including postpartum endometritis, septic abortion, and post-gynecological surgery infections. - Acute gynecological infections. Ertapenem is also used in adults for the prevention of surgical site infections after elective colorectal surgery. Treatment: Ertapenem SUN is indicated for use in children aged 3 months to 17 years and in adults for the treatment of the following infections caused by bacteria known or highly susceptible to ertapenem, requiring parenteral administration (see Sections 4.4 and 5.1): - Intra-abdominal infections - Community-acquired pneumonia - Acute gynecological infections - Diabetic foot skin and soft tissue infections (see Section 4.4). Prevention: Ertapenem SUN is indicated for the prevention of surgical site infections after elective colorectal surgery in adults (see Section 4.4). Official guidelines on the rational use of antimicrobial agents should be consulted. Treatment: When caused by bacteria known or highly susceptible to ertapenem and requiring parenteral administration, the following infections can be treated: intra-abdominal infections; community-acquired pneumonia; acute gynecological infections; diabetic foot skin and soft tissue infections. Prevention: Invanz is indicated for the prevention of surgical site infections after elective colorectal surgery in adults. Official guidelines on the rational use of antimicrobial drugs should be consulted.

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Mechanism of Action
Ertapene has bactericidal activity. Its mechanism of action is through binding to and inhibiting the activity of bacterial penicillin-binding proteins (PBPs). In Escherichia coli, ertapenem has a strong affinity for penicillin-binding proteins (PBPs) 1a, 1b, 2, 3, 4, and 5, especially preferentially binding to PBPs 2 and 3. After binding to PBPs, ertapenem interferes with the elongation and reinforcement of the peptidoglycan moiety of the cell wall, thereby inhibiting bacterial cell wall synthesis.
Ertapene is a synthetic carbapenem β-lactam antibiotic, and its structure and pharmacological action are related to imipenem and meropenem. Similar to meropenem, but unlike imipenem, ertapenem has a methyl group at the 1-position of its five-membered ring, which makes it resistant to hydrolysis by dehydropeptidase 1 (DHP-1) on the brush border of proximal renal tubular cells, thus eliminating the need for co-administration with DHP-1 inhibitors such as cilastatin. Ertapenem exhibits in vitro activity against Gram-positive, Gram-negative aerobic, and anaerobic bacteria. Its bactericidal activity stems from its inhibition of cell wall synthesis and its action through binding to penicillin-binding proteins (PBPs). In Escherichia coli, this compound shows a strong affinity for PBPs 1a, 1b, 2, 3, 4, and 5, with a particular preference for PBPs 2 and 3. Antibacterial drugs are the most common class of drugs that induce epilepsy, with β-lactam antibiotics being the most prevalent. The epileptogenic potential of carbapenems may be directly related to their β-lactam ring structure. Data on individual carbapenems and epileptic activity are scarce. To assess the existing evidence linking carbapenems to epileptic activity, researchers searched the MEDLINE (1966–May 2010), EMBASE (1974–May 2010), and International Pharmaceutical Abstracts (1970–May 2010) databases. References for retrieved articles were also reviewed. Mechanistically, the epileptogenic tendency of β-lactam antibiotics is related to their binding to γ-aminobutyric acid (GABA) receptors. Numerous reports exist of imipenem-cilastatin-induced seizures, with incidence rates ranging from 3% to 33%. Meropenem, doripenem, and ertapenem all have seizure rates below 1%. However, the incidence may increase with increased use of these drugs and their application in new patient populations. High-dose treatment, particularly in patients with renal insufficiency, a history of central nervous system abnormalities, or a history of epilepsy, increases the risk of seizures.

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- Mechanism of action: Ertapenem irreversibly inhibits penicillin-binding proteins (PBPs), disrupting peptidoglycan cross-links and leading to bacterial cell lysis [1,2]
- Clinical indications: Approved for the treatment of complicated intra-abdominal infections, skin/skin and soft tissue infections, and community-acquired pneumonia caused by susceptible pathogens [1,2]
- Limitations: Ineffective against Pseudomonas aeruginosa or Enterococcus faecalis [1,2]

C22H25N3O7S

475.5

475.141

C, 55.57; H, 5.30; N, 8.84; O, 23.55; S, 6.74

153832-46-3

Ertapenem sodium;153773-82-1;Ertapenem disodium;153832-38-3

150610

Solid powder

1.6±0.1 g/cm3

813.9±65.0 °C at 760 mmHg

230-234

446.0±34.3 °C

0.0±3.1 mmHg at 25°C

1.700

-1.07

5

9

7

33

893

6

S([C@@H]1CN[C@H](C(NC2=CC=CC(C(=O)O)=C2)=O)C1)C1=C(C(=O)O)N2C([C@]([H])([C@@H](C)O)[C@@]2([H])[C@H]1C)=O

JUZNIMUFDBIJCM-ANEDZVCMSA-N

InChI=1S/C22H25N3O7S/c1-9-16-15(10(2)26)20(28)25(16)17(22(31)32)18(9)33-13-7-14(23-8-13)19(27)24-12-5-3-4-11(6-12)21(29)30/h3-6,9-10,13-16,23,26H,7-8H2,1-2H3,(H,24,27)(H,29,30)(H,31,32)/t9-,10-,13+,14+,15-,16-/m1/s1

(4R,5S,6S)-3-[(3S,5S)-5-[(3-Carboxyphenyl)carbamoyl]pyrrolidin-3-yl]sulfanyl-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid

MK 826; L-749345; MK-826; Ertapenem; 153832-46-3; (4R,5S,6S)-3-[(3S,5S)-5-[(3-carboxyphenyl)carbamoyl]pyrrolidin-3-yl]sulfanyl-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid; G32F6EID2H; CHEBI:404903; (1R,5S,6S,8R,2'S,4'S)-2-(2-(3-carboxyphenylcarbamoyl)pyrrolidin-4-ylthio)-6-(1-hydroxyethyl)-1-methylcarbapenem-3-carboxylic acid; DTXSID50165456; (4R,5S,6S)-3-((3S,5S)-5-((3-carboxyphenyl)carbamoyl)pyrrolidin-3-ylthio)-6-((R)-1-hydroxyethyl)-4-methyl-7-oxo-1-aza-bicyclo[3.2.0]hept-2-ene-2-carboxylic acid; L749345; MK826; L 749345; MK-0826; MK 0826; MK0826; Ertapenem Sodium; Trade Name: Invanoz; Invanz

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.)