| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| ln Vitro |
AMG133 is a potent GLP-1R agonist with EC50 values of 24.4 pM, 5.7 pM, 123 pM and 2.4 pM for human GLP-1R, cynomolgus monkey GLP-1R, mouse GLP-1R and rat GLP-1R, respectively[1]. AMG133 is also a GIPR antagonist with IC50 values of 42.4 nM, 26.5 nM and 822.3 nM for human GIPR, cynomolgus monkey GIPR and rat GIPR, respectively[1].
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| ln Vivo |
AMG 133 rodent substitutes (2.0 mg/kg; intraperitoneal injection; single dose) caused rapid and sustained weight loss in male db/db mice and steadily reduced blood glucose levels [1]. AMG 133 rodent substitutes (0.5–2.5 mg/kg; intraperitoneal injection; once every 6 days; for a total of 3 doses) caused sustained, dose-dependent weight loss in diet-induced obese male mice, while reducing food intake and improving metabolic parameters [1]. AMG133 (0.25–0.75 mg/kg; subcutaneous injection; once a week; for 6 weeks) reduced the weight of obese male cynomolgus monkeys by 11% and 13% (relative to baseline), respectively, while reducing energy intake and improving metabolic parameters [1].
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| Animal Protocol |
Animal/Disease Models:C57BL/6N (male, 22 weeks old, diet-induced obesity) [1]
Doses: 0.5 mg/kg; 2.5 mg/kg Route of Administration: Intraperitoneal injection; once every 6 days; for 18 days Experimental Results: From day 1 to day 18, body weight decreased significantly in a dose-dependent manner. Food intake also decreased proportionally to the dose, with the most significant decrease on days 0-3. Compared with the control group, blood glucose, plasma insulin, triglycerides and total cholesterol levels were significantly reduced. Animal/Disease Models:Crab-eating macaque (male, BMI > 41 kg/m2, spontaneously obese)[1] Doses: 0.25 mg/kg; 0.75 mg/kg Route of Administration: Subcutaneous injection; once a week for 6 weeks Experimental Results: After 6 weeks of treatment, body weight decreased by 11% (0.25 mg/kg group) and 13% (0.75 mg/kg group) from baseline, respectively. A dose-dependent decrease in total energy intake was observed in the first 3 weeks of administration. Fasting triglycerides, fasting insulin, total cholesterol and low-density lipoprotein cholesterol levels were significantly lower than baseline in both dosage groups. |
| References |
| Molecular Formula |
C196H290BRN55O69.XC2HF3O2
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|---|---|
| Molecular Weight |
4600.70 (free base)
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| Related CAS # |
AMG133 peptide payload
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| Sequence |
His-{Aib}-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ser-Tyr-Leu-Glu-Glu-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Gly-Gly-Gly-Gly-Gly-Gly-Ser-Gly-Gly-Gly-Gly-Ser-Gly-Gly-Gly-Gly-Ser-Lys(BrAc)-NH2H-{Aib}-EGTFTSDYSSYLEEQAAKEFIAWLVKGGGGGGGSGGGGSGGGGS-Lys(BrAc)-NH2
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| SequenceShortening |
H-{Aib}-EGTFTSDYSSYLEEQAAKEFIAWLVKGGGGGGGSGGGGSGGGGS-Lys(BrAc)-NH2
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| Appearance |
White to off-white solid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: 请将本产品存放在密封保护的环境中，避免受潮。 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 50 mg/mL
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| Solubility (In Vivo) |
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.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] Oral Formulations
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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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