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抑制剂描述:

产品名称:YC-1

产品别名:见爱必信官网

英文别名:YC-1

靶点:Guanylate Cyclase

CAS:170632-47-0

纯度:>98%

外观:见爱必信官网

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.

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。

溶解性:DMSO :60 mg/mL (197.14 mM)
Ethanol :60 mg/mL (197.14 mM)

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.

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.

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