AMG133 peptide payload
Based on 1 Customer Validation
AMG133 peptide payload is a GLP-1 analog agonist peptide. AMG133 peptide potently activates GLP-1R, and exhibits weight loss and metabolic improvement activities. AMG133 peptide payload can be used for the synthesis of AMG 133 (HY-164535).
For research use only. We do not sell to patients.
- Purity : 99.94%
- CAS No.: 3137854-22-6
- Formula: C196H290BrN55O69
- Molecular Weight:4600.70
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
AMG133 is a potent GLP-1R agonist, with EC50 values of 24.4 pM, 5.7 pM, 123 pM and 2.4 pM against human GLP-1R, cynomolgus monkey GLP-1R, mouse GLP-1R and rat GLP-1R, respectively[1].
AMG133 acts as a GIPR antagonist, with IC50 values of 42.4 nM, 26.5 nM, and 822.3 nM against human GIPR, cynomolgus monkey GIPR, and rat GIPR, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
AMG 133 murine surrogate (0.5-2.5 mg/kg; i.p.; every 6 days; 3 doses total) induces dose-dependent body weight loss, reduced food intake, and improved metabolic markers in male diet-induced obese mice[1].
AMG133 (0.25-0.75 mg/kg; s.c.; once weekly; 6 weeks) reduces body weight by 11% and 13% respectively relative to baseline in obese male cynomolgus monkeys, while also decreasing energy intake and improving metabolic markers[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6N (male, 22 weeks of age, diet-induced obese)[1]
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Dosage:0.5 mg/kg; 2.5 mg/kg
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Administration:i.p.; every 6 days; 3 doses total
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Result:Produced significant body weight loss from day 1 through day 18, with a dose-dependent effect.
Reduced food intake in a dose-proportional manner, with the most pronounced reduction observed on days 0-3.
Induced significant decreases in blood glucose, plasma insulin, triglycerides, and total cholesterol compared to controls.
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Animal Model:Macaca fascicularis (male, body weight >7 kg, BMI >41 kg/m2, spontaneous obese)[1]
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Dosage:0.25 mg/kg; 0.75 mg/kg
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Administration:s.c.; once weekly; 6 weeks
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Result:Reduced body weight by 11% (0.25 mg/kg dose) and 13% (0.75 mg/kg dose) from baseline after 6 weeks of treatment.
Observed dose-dependent reduction in total energy intake in the first 3 weeks of dosing.
Significantly reduced fasting triglycerides, fasting insulin, total cholesterol, and low-density lipoprotein cholesterol levels from baseline in both dose groups.
Chemical Information
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CAS No. 3137854-22-6
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Appearance Solid
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Molecular Weight 4600.70
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Formula C196H290BrN55O69
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Color White to off-white
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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)-NH2
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Sequence Shortening
H-{Aib}-EGTFTSDYSSYLEEQAAKEFIAWLVKGGGGGGGSGGGGSGGGGS-Lys(BrAc)-NH2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : ≥ 50 mg/mL (10.87 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (0.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (0.54 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (313 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.2174 mL | 1.0868 mL | 2.1736 mL | 5.4340 mL |
| 5 mM | 0.0435 mL | 0.2174 mL | 0.4347 mL | 1.0868 mL | |
| 10 mM | 0.0217 mL | 0.1087 mL | 0.2174 mL | 0.5434 mL |
AMG133 peptide payload Related Classifications
HY-P10736 Related Classifications
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