646995-35-9

中文名称:

646995-35-9

中文同义词:

英文名称:

BAY 58-2667 hydrochloride

英文同义词:

Cinaciguat (hydrochloride);Cinaciguat HCl;4-[[(4-Carboxybutyl)[2-[2-[[4-(2-phenylethyl)phenyl]methoxy]phenyl]ethyl]amino]methyl]benzoic acid hydrochloride;BAY 58-2667 hydrochloride - Cinaciguat hydrochloride;Cinaciguat hydrochloride >=98% (HPLC)

CAS号:

646995-35-9

分子式:

分子量:

0

EINECS号:

相关类别:

API

Mol文件:

Mol File

储存条件 

-20°C

形态

powder

颜色

white to beige

生物活性

Cinaciguat hydrochloride 是一种有效的可溶性鸟苷酸环化酶 (GC) 活化剂，在血小板中 EC50 值为 15 nM。

靶点

EC50:15 nM (Guanylate cyclase)

体外研究

In platelets, Cinaciguat (BAY 58-2667) is a potent GC activator (EC 50 15 nM) but the maximum effect is only about 1% of that achievable with NO. Concentration-response curves for Cinaciguat are constructed after 1 min exposure in the presence of sildenafil. Without ODQ, the EC 50 is 18 nM, and in the presence of ODQ the potency of Cinaciguat is not significantly different, the EC 50 being 13 nM. The potency of Cinaciguat in platelets (EC 50 15 nM) is very similar to estimates made on purified recombinant GC. Cinaciguat at a maximally effective concentration of 1 μM stimulates control GC activity to about 25% of that observed with NO and, contrasting with the stimulation by NO, this level of activity remained constant as the proportion of ODQ-pretreated GC is increased.

体内研究

Administration of Cinaciguat decreased BP and increased HR in both apo-sGC mice and WT mice. In fact, the BP-lowering effect of Cinaciguat in apo-sGC mice is significantly greater and longer lasting than in WT mice. In addition, Cinaciguat decreased BP in apo-sGC mice at concentrations that did not affect BP in WT mice. Furthermore, the IC 50 values for Cinaciguat-induced ex vivorelaxation of precontracted aortas are threefold lower in apo-sGC mice than in WT mice (IC 50 =0.2 nM and 0.7 nM, respectively). Together, our results suggest that sGC activators like Cinaciguat but not sGC stimulators like BAY 41-2272 activate apo-sGC. In addition, the observation that Cinaciguat can modulate vasorelaxation and BP in WT mice suggests that even in healthy mice, a subset of the available sGC pool is haem-free and responsive to sGC activators.