646995-35-9
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- CAS号:
- 646995-35-9
- 英文名:
- BAY 58-2667 hydrochloride
- 英文别名:
- 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
- 中文名:
- 646995-35-9
- 中文别名:
- 化合物 T1984L;BAY 58-2667盐酸盐
- CBNumber:
- CB33146261
- 分子式:
- C36H40ClNO5
- 分子量:
- 602.17
- MOL File:
- 646995-35-9.mol
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646995-35-9化学性质
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储存条件:
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-20°C
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溶解度:
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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)-
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形态:
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powder
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颜色:
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white to beige
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646995-35-9性质、用途与生产工艺
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。
EC50:15 nM (Guanylate cyclase)
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.
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.
646995-35-9
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上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-14181A | 646995-35-9 Cinaciguat hydrochloride | 646995-35-9 | 2mg | 1100元 |
2024/04/30 | HY-14181A | 646995-35-9 Cinaciguat hydrochloride | 646995-35-9 | 5mg | 1650元 |
646995-35-9, 646995-35-9 相关搜索:
- API
- BAY 58-2667盐酸盐
- 化合物 T1984L
- 646995-35-9
- 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
- Cinaciguat HCl
- Cinaciguat (hydrochloride)