158001-76-4
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- CAS号:
- 158001-76-4
- 英文名:
- Win 58237
- 英文别名:
- Win 58237;4H-Pyrazolo[3,4-d]pyrimidin-4-one, 1-cyclopentyl-1,5-dihydro-3-methyl-6-(4-pyridinyl)-
- 中文名:
- 158001-76-4
- 中文别名:
- 化合物 T13341
- CBNumber:
- CB13175603
- 分子式:
- C16H17N5O
- 分子量:
- 295.34
- MOL File:
- 158001-76-4.mol
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158001-76-4化学性质
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密度:
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1.46±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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7.77±0.20(Predicted)
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158001-76-4性质、用途与生产工艺
Win 58237 是一种 phosphodiesterase (PDE) 抑制剂,对 PDE V 有很强的亲和力,Ki 值为 170 nM,具有舒张血管的作用。
Win 58237 is a competitive inhibitor of cGMP PDE V from canine aorta, with a K
i
value of 170 nM. Win 58237 is a potent inhibitor of PDE V isolated from vascular tissue with an IC
50
value of 240 nM. It is a relatively less potent inhibitor of calmodulin-sensitive PDE I and cGMP-inhibitable cyclic AMP PDE III; but does inhibit cyclic AMP PDE IV with an IC
50
value of approximately 300 nM. Win 58237 possesses vasorelaxant activity in the presence of an intact endothelium or nitric oxide.
Win 58237 (0.3-3.0 mg/kg i.v.) decreases mean arterial pressure in conscious spontaneously hypertensive rats with an associated increase in vascular (aortic) cGMP content in vivo. Win 58237 (10 mg/kg i.v.) increases plasma cGMP levels, from basal levels of 6.7 ± 1.0 to 31.4 ± 3.5 fmol/μL.
158001-76-4
上下游产品信息
上游原料
下游产品
158001-76-4, 158001-76-4 相关搜索:
- 化合物 T13341
- 158001-76-4
- 4H-Pyrazolo[3,4-d]pyrimidin-4-one, 1-cyclopentyl-1,5-dihydro-3-methyl-6-(4-pyridinyl)-
- Win 58237