VU0071063

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

VU0071063 是 Kir6.2/SUR1 激活剂。

VU0071063 is a Kir6.2/SUR1 activator.

VU0071063 (1 nM~1 mM; HEK-293 cells) dose dependently opens Kir6.2/SUR1. VU0071063 (0~20 μM; isolated cells) inhibits β-Cell excitability in mouse Islets. VU0071063 (10 μM; 1 hour; isolated cells) inhibits glucose-stimulated insulin secretion.VU0071063 dose dependently and reversibly hyperpolarizes the β-cell membrane potential, which, in turn, inhibits glucose-stimulated Ca2+ entry and insulin secretion. The actions of VU0071063 on the β-cell membrane potential are reversed by tolbutamide, and glucose stimulated insulin secretion is unaffected by the inactive analog 34MT, indicating that the effects are mediated through Kir6.2/SUR1.

VU0071063 (50 mg/kg; i.p.; 4 hours) leads to a significant increase in blood glucose at 60 minutes. Animal Model:Male C57BL/6 mice (10-12 weeks age)Dosage:50 mg/kg (Pharmacokinetic analysis)Administration: I.p.Result:Led to a significant increase in blood glucose at 60 minutes.

VU-0071063 | VU 0071063

Cell Cycle/DNA Damage

Potassium Channel

Kir6.2/SUR1

——

——

333415-38-6

326.4

C18H22N4O2

>98% (HPLC)

DMSO:10 mM

O=C(N1C)N(C)C2=C(N(CC3=CC=C(C(C)(C)C)C=C3)C=N2)C1=O

——

(-20℃)

With Ice Pack

≥ 2 years