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223645-67-8

中文名稱 Ripasudil
英文名稱 Ripasudil
CAS 223645-67-8
分子式 C15H18FN3O2S
更新日期 2024/12/23 09:09:16
分子量 323.39
MOL 文件 223645-67-8.mol
223645-67-8 結(jié)構(gòu)式 223645-67-8 結(jié)構(gòu)式

基本信息

中文別名
瑞舒地爾
化合物BAY 41-2272
英文別名
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]-

物理化學(xué)性質(zhì)

沸點(diǎn)497.2±55.0 °C(Predicted)
密度1.293±0.06 g/cm3(Predicted)
儲(chǔ)存條件under inert gas (nitrogen or Argon) at 2–8 °C
溶解度Soluble in DMSO
酸度系數(shù)(pKa)9.70±0.40(Predicted)
形態(tài)powder
顏色white to beige
水溶解性H2O: 2mg/mL, clear
InChI1S/C15H18FN3O2S/c1-11-8-17-6-3-7-19(11)22(20,21)14-5-2-4-12-9-18-10-13(16)15(12)14/h2,4-5,9-11,17H,3,6-8H2,1H3/t11-/m0/s1
InChIKeyQSKQVZWVLOIIEV-NSHDSACASA-N
SMILESFc1c2c(cnc1)cccc2[S](=O)(=O)N3[C@H](CNCCC3)C

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)有害 (GHS07)
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
WGK GermanyWGK 3
存儲(chǔ)類別11 - Combustible Solids
Ripasudil價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2025/12/22HY-15685Ripasudil
Ripasudil
223645-67-82mg1060元
2025/12/22HY-15685Ripasudil
Ripasudil
223645-67-85mg1600元
2025/12/22HY-15685Ripasudil
Ripasudil
223645-67-810 mM * 1 mLin DMSO1760元

常見問題列表

生物活性
Ripasudil free base (K-115 free base) 是 ROCK 特異性抑制劑,能夠抑制 ROCK2 和 ROCK1 的活性,IC50 值分別為 19 和 51 nM。
靶點(diǎn)

ROCK2

19 nM (IC 50 )

ROCK1

51 nM (IC 50 )

CaMKIIa

370 nM (IC 50 )

PKACa

2.1 μM (IC 50 )

PKC

27 μM (IC 50 )

體外研究

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.

體內(nèi)研究

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.

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