CAS:170632-47-0Lificiguat

Synonyms: Lificiguat

Lificiguat is an acivator of guanylyl cyclase (sGC) and can bind to the heme-containing domain of the β subunit with Kd of 0.6 μM - 1.1 μM.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

技术信息

CAS号

170632-47-0

储存条件

分子式

C19H16N2O2

运输

蓝冰

分子量

304.34

别名

Lificiguat

溶解度

DMSO	160.0 mg/mL (525.7 mM)
Water	insoluble

动物实验配方

生物活性

描述YC-1 is an allosteric activator of soluble guanylyl cyclase (sGC). YC-1 exerts antiplatelet effects through the sGC/cyclic GMP pathway. It increased the catalytic rate of the enzyme and sensitizes the enzyme toward its gaseous activators nitric oxide or carbon monoxide. YC-1 activation of sGC can occur independently of heme, but that activation is substantially increased when the heme moiety is present in the enzyme. Administration of YC-1 to experimental animals resulted in the inhibition of the platelet-rich thrombosis and a decrease of the mean arterial pressure, which correlated with increased cGMP levels.
作用机制YC-1 increases the maximal catalytic rate and sensitizes the enzyme toward its gaseous activators by binding to an allosteric site on sGC molecules, thereby reducing the ligand dissociation rate from the heme group.^[3]
动物研究
剂量
Mice: 30 mg/kg, 60 mg/kg^[4] (i.p.); 6.96 mg/kg^[5] (i.v.) Rat: 1 mg/kg^[6] (i.p.)

给药途径
i.p., i.v.

动物研究
剂量	Mice: 30 mg/kg, 60 mg/kg^[4] (i.p.); 6.96 mg/kg^[5] (i.v.) Rat: 1 mg/kg^[6] (i.p.)
给药途径	i.p., i.v.