DJ-V159

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

DJ-V159 是 G 蛋白偶联受体家族 C 组 6 成员 A (GPRC6A) 的激动剂。

DJ-V159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).

DJ-V-159 activates ERK in HEK-293 transfected with GPRC6A but not in non-transfected HEK-293 cells, with potency similar to L-Arg. In addition, DJ-V-159 dose-dependently stimulates cAMP production in GPRC6A expressing HEK-293 cells, achieving a response a 0.2 nM concentrations in the media. DJ-V-159 stimulates insulin secretion in mouse beta-cell MIN-6 cells. The DJ-V-159 increased insulin stimulation index (SI) in MIN-6 cells similar to the effects of Ocn, known ligand of GPRC6A.

DJ-V-159 at the dose of 10 mg/kg reduces blood glucose levels in wildtype mice at 60 and 90 minutes after intraperitoneal administration of 10 mg/kg, whereas the vehicle (95% PEG + 5% DMSO) has no effect on blood glucose. DJ-V-159 reduces blood glucose levels in wild-type mice by 43.6% and 41.9% at 60 and 90 minutes, respectively, after intraperitoneal administration of 10 mg/kg. The mice tolerated this short-term exposure to DJ-V-159 without any overt side-effects. DJ-V-159, however, is almost in or on the boundary of the Lipinski's Rule of Five.

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Cell Cycle/DNA Damage

GPR

GPRC6A

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2253744-53-3

502.37

C24H12F6N4O2

>98% (HPLC)

DMSO: 10 mg/mL

FC(F)(F)c1cc(NC(=O)c2cccc(c2)C(=O)Nc2ccc(C#N)c(c2)C(F)(F)F)ccc1C#N

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(-20℃)

With Ice Pack

≥ 2 years