Ripasudil
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- CAS号:
- 223645-67-8
- 英文名:
- Ripasudil
- 英文别名:
- CS-1564;Ripasudil;k115 free base;K-115, Ripasudil;RIPASUDIL HYDROCHLOIDE;RIPASUDIL FREE BASE;K 115 FREE BASE;K115 FREE BASE;4-Fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]isoquinoline;Isoquinoline, 4-fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]-
- 中文名:
- Ripasudil
- 中文别名:
- 瑞舒地尔;化合物BAY 41-2272;(S)-4-氟-5-((2-甲基-1,4-二氮杂卓-1-基)磺酰基)异喹啉
- CBNumber:
- CB92722374
- 分子式:
- C15H18FN3O2S
- 分子量:
- 323.39
- MOL File:
- 223645-67-8.mol
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Ripasudil化学性质
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沸点:
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497.2±55.0 °C(Predicted)
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密度:
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1.293±0.06 g/cm3(Predicted)
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储存条件:
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under inert gas (nitrogen or Argon) at 2–8 °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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9.70±0.40(Predicted)
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Ripasudil性质、用途与生产工艺
Ripasudil free base (K-115 free base) 是 ROCK 特异性抑制剂，能够抑制 ROCK2 和 ROCK1 的活性，IC50 值分别为 19 和 51 nM。
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ROCK2
19 nM (IC
50
)
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ROCK1
51 nM (IC
50
)
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CaMKIIa
370 nM (IC
50
)
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PKACa
2.1 μM (IC
50
)
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PKC
27 μM (IC
50
)
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Ripasudil (K-115) is a potent inhibitor of ROCK, with IC
50
s of 19 and 51 nM for ROCK2 and ROCK1, respectively. Ripasudil also shows less potent inhibitory activities against CaMKIIα, PKACα and PKC, with IC
50
s of 370 nM, 2.1 μM and 27 μM, respectively. Ripasudil (K-115; 1, 10 μM) induces cytoskeletal changes, including retraction and cell rounding and reduced actin bundles of cultured trabecular meshwork (TM) cells. Ripasudil (5 μM) sifnificantly reduces transendothelial electrical resistance (TEER), and increases FITC-dextran permeability in Schlemm’s canal endothelial (SCE) cell monolayers.
Ripasudil (K-115) reduces intraocular pressure (IOP) in a concentration-dependent manner at concentrations between 0.1% and 0.4% in monkey eyes and 0.0625% to 0.5% in rabbit eyes, respectively. Ripasudil (K-115; 1 mg/kg, p.o. daily) shows a neuroprotective effect on retinal ganglion cells (RGCs) after nerve crush (NC). Ripasudil also inhibits the oxidative stress induced by axonal injury in mice. Ripasudil suppresses the time-dependent production of ROS in RGCs after NC injury.
Ripasudil
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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 |
|---|
| 2024/04/30 | HY-15685 | Ripasudil
Ripasudil | 223645-67-8 | 5mg | 1600元 |
| 2024/04/30 | HY-15685 | Ripasudil
Ripasudil | 223645-67-8 | 10 mM * 1 mLin DMSO | 1760元 |
223645-67-8, Ripasudil 相关搜索:
- 对照品
- 原料药
- (S)-4-氟-5-((2-甲基-1,4-二氮杂卓-1-基)磺酰基)异喹啉
- 化合物BAY 41-2272
- 瑞舒地尔
- 223645-67-8
- RIPASUDIL HYDROCHLOIDE
- Isoquinoline, 4-fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]-
- K-115, Ripasudil
- CS-1564
- RIPASUDIL FREE BASE;K 115 FREE BASE;K115 FREE BASE
- 4-Fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]isoquinoline
- Ripasudil
- k115 free base