BETP

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BETP 是 GLP-1 受体的激动剂（EC50：人和大鼠 GLP-1 受体的 EC50 分别为 0.66 和 0.755 μM）。

BETP is an agonist of GLP-1 receptor (EC50s: 0.66 and 0.755 μM for human and rat GLP-1 receptor).

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.

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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GPCR/G Protein

Glucagon Receptor

GLP-1

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1371569-69-5

406.42

C20H17F3N2O2S

>98% (HPLC)

DMSO:25 mg/mL (61.51 mM; Need ultrasonic);Water:Insoluble

CCS(c1nc(-c2cc(OCc3ccccc3)ccc2)cc(C(F)(F)F)n1)=O

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(-20℃)

With Ice Pack

≥ 2 years