GV-58 是选择性 N 型和 P/Q 型 Ca2+ 通道激动剂，EC50值分别为7.21和8.81uM。它对 CDK 激酶活性的抑制作用减少了 20 倍。

GV-58 is a selective N- and P/Q-type Ca2+ channels agonist (EC50: 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel). The inhibitory of GV-58 is 20-fold fewer for CDK kinases activity.

In comparison with the parent molecule, (R)-roscovitine, GV-58 has a 20-fold less potent cyclin-dependent kinase antagonist effect, a 3- to 4-fold more potent Ca2+ channel agonist effect, and 4-fold higher efficacy as a Ca2+ channel agonist. GV-58 had no agonist activity (up to 100 μm) on the L-type α-subunit we tested (Cav1.3).

1402821-41-3

C18H26N6OS

374.5

DMSO:90 mg/mL (240.32 mM),Need ultrasonic
Methanol:55 mg/mL (146.86 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years