2. GPCR/G Protein
  3. GCGR
  4. AMG133 peptide payload TFA

AMG133 peptide payload TFA is a GLP-1 analog agonist peptide. AMG133 peptide payload TFA potently activates GLP-1R and exhibits weight loss and metabolic improvement activities. AMG133 peptide payload TFA can be used for the synthesis of AMG 133 (HY-164535).

For research use only. We do not sell to patients.

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AMG133 peptide payload TFA

AMG133 peptide payload TFA Chemical Structure

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Other Forms of AMG133 peptide payload TFA:

AMG133 peptide payload TFA Related Antibodies

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Description

AMG133 peptide payload TFA is a GLP-1 analog agonist peptide. AMG133 peptide payload TFA potently activates GLP-1R and exhibits weight loss and metabolic improvement activities. AMG133 peptide payload TFA can be used for the synthesis of AMG 133 (HY-164535)[1].

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.

AMG133 peptide payload TFA Related Antibodies
In Vivo

AMG 133 murine surrogate (2.0 mg/kg; i.p.; single dose) induces rapid and sustained body weight loss, as well as stable blood glucose reduction, in male db/db mice[1].
AMG 133 murine surrogate (0.5-2.5 mg/kg; i.p.; every 6 days; 3 doses total) produces sustained, dose-dependent body weight loss, reduced food intake, and improved metabolic parameters in diet-induced obese male mice[1].
AMG133 (0.25-0.75 mg/kg; s.c.; once weekly; 6 weeks) reduces body weight in obese male cynomolgus monkeys by 11% and 13% relative to baseline levels, respectively, 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.

Animal Model: C57BL/6N (male, 22 weeks of age, diet-induced obese)[1]
Dosage: 0.5 mg/kg; 2.5 mg/kg
Administration: i.p.; every 6 days; 18 days
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.
Animal Model: Macaca fascicularis (male, BMI > 41 kg/m2, spontaneous obese)[1]
Dosage: 0.25 mg/kg; 0.75 mg/kg
Administration: s.c.; once weekly; 6 weeks
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.
Molecular Weight

4600.70 (free base)

Formula

C196H290BrN55O69.xC2HF3O2
Appearance

Solid

Color

White to off-white

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
Sequence Shortening

H-{Aib}-EGTFTSDYSSYLEEQAAKEFIAWLVKGGGGGGGSGGGGSGGGGS-Lys(BrAc)-NH2
Shipping

Room temperature in continental US; may vary elsewhere.
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

*"≥" means soluble, but saturation unknown.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.70%

SDS (252 KB)

COA (275 KB) LCMS (101 KB)

Handling Instructions (2659 KB)
References
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AMG133 peptide payload TFA Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AMG133 peptide payloadGCGRGlucagon Receptorobese male micecynomolgus monkeymale db/db micerat GIPR-expressing cellscynomolgus monkey GLP-1R-expressing cellsGIPRInhibitorinhibitorinhibit

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AMG133 peptide payload TFA
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HY-P10736A
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