P d D Sh Product Name:
ROCK inhibitor CAS No.:
867017-68-3Cat. No.:
HY-10319
Product Data Sheet
MWt:
402.79Formula:
C18H13ClF2N6O Purity :>98%
Solubility:
DMSO
Mechanisms:Biological Activity:
ROCK inhibitor(azaindole 1) is a highly potent inhibitor of human ROCK-1 and ROCK-2 isoenzymes
Pathways:Cell Cycle/DNA Damage; Target:ROCK Pathways:TGF-beta/Smad; Target:ROCK ()g y p y
with IC50 values of 0.6 and 1.1 nM, respectively.
IC50 value: 0.6 nM(ROCK1); 1.1 nM (ROCK2) [1]
Target: ROCK in vitro: ROCK inhibitor is a highly potent inhibitor of human ROCK-1 and ROCK-2 isoenzymes with IC50 values of 0.6 and 1.1 nM, respectively. Azaindole 1 inhibited concentration dependently the phenylephrine-induced contraction of rabbit saphenous artery with an IC50 value of 65 nM. In contrast, the ROCK inhibitor Y-27632 relaxed precontracted saphenous artery with an IC50 of 1.5
uM [1].i i I t i t i d l 1l i d d d d d t d i t t d i References:
[1]. Kast, R.; Schirok, H.; Figueroa-Perez, S.; Mittendorf, J.; Gnoth, M. J.; Cardiovascular effects of a novel potent and highly selective azaindole-based inhibitor of Rho-kinase. British Journal of Pharmacology (2007)152(7)10701080in vivo: In normotensive rats, azaindole 1 also induced a dose dependent and persistent decrease in blood pressure. After oral administration of 3 and 10 mg/kg, mean blood pressure dropped by 20mm Hg (13%) and 41 mm Hg (40%), respectively. The effect lasted approximately 10 h after ...Pharmacology (2007), 152(7), 1070-1080.
Caution: Not fully tested. For research purposes only
Medchemexpress LLC
https://www.doczj.com/doc/036567248.html,
18W i l k i n s o n W a y , P r i n c e t o n , N J 08540,U S A
E m a i l : i n f o @m e d c h e m e x p r e s s .c o m W e b : w w w .m e d c h e m e x p r e s s .c o m