GV-58

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

GV-58 是一种有效的选择性 N 型和 P/Q 型 Ca2+ 通道激动剂，EC50 分别为 7.2 和 8.8 uM。

GV-58 is a potent, selective N-Type and P/Q-type Ca2+ Channel agonist with EC50 of 7.2 and 8.8 uM, shows no acitivity for L-type calcium channels (EC50>100 uM); has 20-fold less potent cyclin-dependent kinase antagonist effect; slows deactivation (closing) of the channel, resulting in a large increase in total calcium entry during motor nerve action potential activity; weakens Lambert-Eaton myasthenic syndrome-model neuromuscular synapses in a passive transfer mouse model of Lambert-Eaton myasthenic syndrome.

GV-58 (50 μM; 30 min) restores function in LEMS passive transfer neuromuscular junction. Cell Viability Assay Cell Line:Upper arm muscle isolated from LEMS mice Concentration:50 μM Incubation Time:30 min Result:Increased the mEPP frequency from 3.27 s?1 in vehicle controls to 10.45 s?1. Showed a slight facilitation followed by depression to ～94% at the final EPP in the train.

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GV58

GPCR/G Protein

Calcium Channel

Calcium Channel

Neurological Disease

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1402821-41-3

374.5036

C18H26N6OS

>98% (HPLC)

10 mM in DMSO

CCCN1C=NC2=C(N=C(N=C21)NC(CC)CO)NCC3=CC=C(S3)C

1-Butanol, 2-[[6-[[(5-methyl-2-thienyl)methyl]amino]-9-propyl-9H-purin-2-yl]amino]-, (2R)-

(-20℃)

With Ice Pack

≥ 2 years