KB-1208

AMG133-GIPR-hIgG1

12209

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Background of AMG133-GIPR-hIgG1

AMG133 is a bispecific glucose-dependent insulinotropic polypeptide receptor (GIPR) antagonist and glucagon-like peptide-1 (GLP-1) receptor agonist molecule. AMG133 mimics the agonist effects of GLP-1 and antagonizes the effects of glucose-dependent insulinotropic polypeptide (GIP). Amgen moved into this Phase 1 study based on human genetic insights and preclinical evidence that suggested synergistic effects with GIP receptor blockade and GLP-1 receptor agonism on weight loss and improvement in other metabolic parameters.

Specifications

Catalog Number	KB-1208
Antibody Name	AMG133-GIPR-hIgG1
Isotype	Human IgG1,kappa
FC Muations	S228P/L235E
Target	GIPR
Species Reactivity	Human
Host Cell Line	EXPI CHO
Purification Method	Affinity purified
Concentration	>2 mg/mL
Formulation	50 mM sodium citrate,150mM NaCl,pH5.5
Purity	>95% by SDS-PAGE and SEC-HPLC
Validation	ELISA
Endotoxin Level	<0.2 EU/mg as determined by the LAL method
Sterility	0.2μm filtered
Storage	It is recommended that the protein should be aliquoted for optimal storage. Avoid repeated freeze-thaw cycles.
Stability	Stable for twelve months from date of receipt when stored at -20°C to -80°C; Stored at 2-8°C for one month without detectable loss of activity.

Characterization

Application

References

Véniant MM, Lu SC, Atangan L, Komorowski R, Stanislaus S, Cheng Y, Wu B, Falsey JR, Hager T, Thomas VA, Ambhaikar M, Sharpsten L, Zhu Y, Kurra V, Jeswani R, Oberoi RK, Parnes JR, Honarpour N, Neutel J, Strande JL. A GIPR antagonist conjugated to GLP-1 analogues promotes weight loss with improved metabolic parameters in preclinical and phase 1 settings. Nat Metab. 2024 Feb;6(2):290-303.
Dose-ranging Study to Evaluate the Efficacy, Safety, and Tolerability of AMG 133 in Adult Subjects With Overweight or Obesity, With or Without Type 2 Diabetes Mellitus-NCT05669599