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BETP

CAS No. : 1371569-69-5

MCE 国际站：BETP

产品活性：BETP 是一种胰高血糖素样肽 (GLP-1) 受体激动剂，对人和大鼠 GLP-1 受体的 EC₅₀ 值分别为 0.66 μM 和 0.755 μM。

研究领域：GPCR/G Protein

作用靶点：GCGR

In Vitro: BETP is a GLP-1 receptor agonist, with EC₅₀s of 0.66 and 0.755 μM for human and rat GLP-1 receptor, respectively. BETP (Compound B) is inactive in cells expressing the GLP-2, GIP, PTH, or glucagon receptors. BETP (1-10 μM) enhances insulin secretion in normal and diabetic human islets. In addition, BETP in combination with GLP-1 shows additive effects on increasing GLP-1 receptor signaling. BETP increases the potency of oxyntomodulin by 10-fold (EC₅₀ of 80 pM). GLP-1 does not change the potencies and efficacies of both oxyntomodulin and glucagon at the glucagon receptor. BETP (0-30 μM) increases the binding affinity of oxyntomodulin for the GLP-1 receptor.

In Vivo: BETP has insulinotropic effect in SD rats. BETP (10 mg/kg, jugular vein cannula) exhibits insulin secretagogue activity in the intravenous glucose tolerance test (IVGTT) model. BETP (10 mg/kg, i.v.)-treated rats need 20% higher glucose infusion rates and demonstrates higher plasma insulin levels in SD rat hyperglycemic clamp model. BETP (5 mg/kg) enhances oxyntomodulin-stimulated insulin secretion.

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