Insulin Receptor Antagonist

Human GIP(3-30), amide is a high affinity antagonist of the human GIP receptor in vitro. Human GIP(3-30), amide has potential anti-obesity and anti-diabetic effects.

S961 acetate is an high-affinity and selective insulin receptor (IR) antagonist with IC₅₀s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively.

Maridebart cafraglutide (AMG 133) is a long-acting peptide-antibody conjugate that combines GLP-1 receptor agonist with glucose-dependent insulinotropic polypeptide (GIP) receptor antagonism. Maridebart cafraglutide shows antagonist activity against human, cynomolgus monkey and rat GIPR with IC₅₀ values of 46.4 nM, 26.5 nM, 822.3 nM, respectively. Maridebart cafraglutide shows agonist activity against human, cynomolgus monkey, rat and mouse GLP-1R with EC₅₀ values of 24.4 pM, 5.7 pM, 2.4 pM and 123 pM, respectively. Maridebart cafraglutide can be used for the study of obesity and type 2 diabetes.

GIP (3-42), human acts as a glucose-dependent insulinotropic polypeptide (GIP) receptor antagonist, moderating the insulin secreting and metabolic actions of GIP in vivo.

Human GIP(3-30), amide TFA is the TFA salt form of human GIP(3-30), amide (HY-P10138). Human GIP(3-30), amide TFA is a high affinity antagonist of the human GIP receptor in vitro. Human GIP(3-30), amide TFA has potential anti-obesity and anti-diabetic effects.

S961 is an high-affinity and selective insulin receptor (IR) antagonist with IC₅₀s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively.

[Pro3]-GIP (mouse) is a GIP receptor antagonist (IC₅₀: 2.6 μM). [Pro3]-GIP (mouse) improves glucose tolerance and insulin sensitivity in ob/ob mice. [Pro3]-GIP (mouse) can be used for research of type 2 diabetes.

β-D-Galactose pentaacetate is a negative regulator of insulin with plasma membrane penetrating ability and can be hydrolyzed by intracellular esterases. β-D-Galactose pentaacetate inhibits Leucine (HY-N0486)-induced insulin release in Wistar rat islets, potentially preventing excessive insulin release in pathological conditions.

IRAB-B is a human monoclonal antibody targeting INSR. IRAB-B is an insulin receptor (IR) antagonist and can be used in the study of insulin resistance and diabetes.

KU14R is a new I(3)-R antagonist, which selectively blocks the insulin secretory response to imidazolines.

S961 TFA is an high-affinity and selective insulin receptor (IR) antagonist with IC₅₀s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively.

XOMA 129 is a human monoclonal antibody targeting INSR. XOMA 129 is an insulin receptor (IR) antagonist that inhibits the drop in blood glucose. XOMA 129 can be used in the study of hypoglycemia .