YC-1

YC-1CAS号: 170632-47-0分子式: C19H16N2O2分子量: 304.34描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述

YC-1(Lificiguat)是一sGC激动剂,结合sGCc的β)亚基heme-containing domain,在CO存在情况下,Kd值为0.6-1.1uM。

纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
利非西呱;Lificiguat;YC1;YC 1
外观
white solid
可溶性/溶解性
DMSO :60 mg/mL (197.14 mM)
Ethanol :60 mg/mL (197.14 mM)
生物活性
靶点
sGC;HIF-1α
In vitro(体外研究)
YC-1 is an allosteric activator of soluble guanylyl cyclase (sGC). YC-1 increases the catalytic rate of the enzyme and sensitizes the enzyme toward its gaseous activators nitric oxide or carbon monoxide. YC-1 alone activates the enzyme only 10-fold, but it potentiates the CO- and NO-dependent activation of sGC, resulting in stimulation of the highly purified enzyme that may be several hundred- to several thousand-fold . It inhibits platelet aggregation and vascular contraction and also inhibits HIF-1 activity in vitro. YC-1 completely blocks HIF-1α expression at the post-transcriptional level and consequently inhibits the transcription factor activity of HIF-1 in hepatoma cells cultured under hypoxic conditions, suggesting that these effects of YC-1 are likely to be linked with the oxygen-sensing pathway and not with the activation of soluble guanylyl cyclase.
In vivo(体内研究)
The administration of YC-1 to experimental animals results in the inhibition of the platelet-rich thrombosis and a decrease of the mean arterial pressure, which correlates with increased cGMP levels . YC-1 effectively inhibits tumor growth in tumor-bearing mice. The inhibition of HIF-1 activity in tumors from YC-1-treated mice is associated with blocked angiogenesis and an inhibition of tumor growth, while the anti-platelet aggregation effect of YC-1 does not appear to affect tumor growt.

分子结构图

YC-1