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646995-35-9

中文名稱 646995-35-9
英文名稱 BAY 58-2667 hydrochloride
CAS 646995-35-9
分子式 C36H40ClNO5
分子量 602.17
MOL 文件 646995-35-9.mol
更新日期 2024/06/25 17:15:55
646995-35-9 結構式 646995-35-9 結構式

基本信息

中文別名
化合物 T1984L
英文別名
Cinaciguat HCl
Cinaciguat (hydrochloride)
Cinaciguat hydrochloride >=98% (HPLC)
BAY 58-2667 hydrochloride - Cinaciguat hydrochloride
4-[[(4-Carboxybutyl)[2-[2-[[4-(2-phenylethyl)phenyl]methoxy]phenyl]ethyl]amino]methyl]benzoic acid hydrochloride

物理化學性質

儲存條件-20°C
溶解度DMSO:66.74(Max Conc. mg/mL);110.83(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);0.83(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);49.82(Max Conc. mM)
Ethanol:5.0(Max Conc. mg/mL);8.3(Max Conc. mM)
形態(tài)粉末
顏色白色至米色
InChIKeyLLHMBJOVHATVSP-UHFFFAOYSA-N
SMILESOC(C(C=C1)=CC=C1CN(CCCCC(O)=O)CCC2=CC=CC=C2OCC3=CC=C(CCC4=CC=CC=C4)C=C3)=O.[H]Cl

安全數(shù)據

WGK GermanyWGK 3
存儲類別11 - Combustible Solids
646995-35-9價格(試劑級)
報價日期產品編號產品名稱CAS號包裝價格
2026/06/05HY-14181AR646995-35-9
Cinaciguat hydrochloride (Standard)
646995-35-91 mg1540元
2026/06/05HY-14181AR646995-35-9
Cinaciguat hydrochloride (Standard)
646995-35-95 mg3080元
2026/06/05HY-14181A646995-35-9
Cinaciguat hydrochloride
646995-35-92mg620元

常見問題列表

生物活性
Cinaciguat hydrochloride 是一種有效的可溶性鳥苷酸環(huán)化酶 (GC) 活化劑,在血小板中 EC50 值為 15 nM。
靶點

EC50:15 nM (Guanylate cyclase)

體外研究

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.

體內研究

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.

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