SAR407899 hydrochloride, Rho- 相关蛋白激酶抑制剂

小分子

SAR407899盐酸盐

923262-96-8 | MS-23990 | SAR-407899 HCl | 1(2H)-Isoquinolinone, 6-(4-piperidinyloxy)-, hydrochloride (1:1) | MFCD20485429 | SAR407899 (hydrochloride) | 6-(piperidin-4-yloxy)-2h-isoquinolin-1-one-hydrochloride | BCP13153 | UNII-AD9C9XVB9T | HY-15687 | 6-(p

SAR407899 hydrochloride

S648099-5mg

5mg

≥98%

2-8°C储存,干燥

冰袋运输

SAR407899 hydrochloride is a selective, potent and ATP-competitive ROCK inhibitor, with an IC 50 of 135 nM for ROCK-2 , and K i s of 36 nM and 41 nM for human and rat ROCK-2 , respectively. In Vitro SAR407899 hydrochloride is a potent and ATP-competitive ROCK inhibitor, with K i s of 36 nM and 41 nM for human and rat ROCK-2, respectively. SAR407899 inhibits ROCK-2 better than ROCK-1, with IC 50 s of 102±19 nM and 276±26 nM, respectively, in the presence of 40 μM ATP. SAR407899 also less potently inhibits PKC-Δ and MSK-1, with IC 50 s of 5.4 and 3.1 μM, respectively. SAR407899 (0.1, 0.3, 1.0, and 3.0 μM) specifically inhibits the ROCK-mediated phosphorylation of MYPT T696 in HeLa cells stimulated with PHEN, and shows such effects at 1 μM and 10 μM in primary rat aortic smooth muscle cells. SAR407899 (3 μM) completely blocks thrombin-induced shrinkage of human umbilical vein endothelial cells (HUVECs) and stress fiber formation. SAR407899 concentration-dependently inhibits 5-bromodeoxyuridine incorporation into the cells with an IC 50 of 5.0±1.3 μM. SAR407899 also effectively inhibits THP-1 migration with an IC 50 of 2.5±1.0 μM. SAR407899 shows a potent vasorelaxant activity in a broad variety of isolated arteries taken from different vascular beds and species, with a range of IC 50 values between 122 and 280 nM. SAR407899 dose-dependently relaxes the phenylephrine pre-contracted smooth muscle, with IC 50 s of 0.07 and 0.05 μM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo SAR407899 (3 mg/kg, i.v.) inhibits ROCK-mediated phosphorylation of MYPT T696 in thoracic aorta of spontaneously hypertensive rats (SHRs). SAR407899 (0.01-0.30 mg/kg, i.v.) efficiently reduces pressor responses to vasoconstrictor agents in rats. SAR407899 (1, 3, 10, and 30 mg/kg, p.o.) dose dependently lowers blood pressure in hypertensive SHRs . SAR407899 (1-3 mg/kg, i.v. or 3, 10 mg/kg, p.o.) increases the length of the penis in healthy rabbits. SAR407899 (3-10 mg/kg, p.o.) also dose-dependently increases penile length in diabetic rabbits. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal administration Rabbits are treated either intravenously (i.v., in an ear vein) with increasing doses of SAR407899 (0.3, 1, 3, 10 mg/kg) or orally with SAR407899 (1, 3, 10, 30 mg/kg) or sildenafil (2 or 6 mg/kg). Each animal is used several times for different doses and different agents, always with a week's washout. The length (mm) of uncovered penile mucosa (penile erection parameter) is measured at different time-points, using a sliding digital caliper. The results are expressed as mean ± SEM penile length of 3-5 rabbits . aladdin has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:ROCK-2 102 nM (IC 50 ) ROCK-1 276 nM (IC 50 )

SAR407899 盐酸盐是一种选择性、强效和 ATP 竞争性 ROCK 抑制剂，对 ROCK-2 的 IC 50 为 135 nM，对人类和大鼠 ROCK-2 的 K i s 分别为 36 nM 和 41 nM。

923262-96-8

C14H17ClN2O2

280.75 g/mol

42635918

C1CNCCC1OC2=CC3=C(C=C2)C(=O)NC=C3.Cl

6-piperidin-4-yloxy-2H-isoquinolin-1-one;hydrochloride

1S/C14H16N2O2.ClH/c17-14-13-2-1-12(9-10(13)3-8-16-14)18-11-4-6-15-7-5-11;/h1-3,8-9,11,15H,4-7H2,(H,16,17);1H

KMNVOGVCCZNVNU-UHFFFAOYSA-N

C1CNCCC1OC2=CC3=C(C=C2)C(=O)NC=C3.Cl

42635918

H2O : 50 mg/mL (178.09 mM; Need ultrasonic) DMSO : 25 mg/mL (89.05 mM; Need ultrasonic)

3

3

2

280.098 Da

280.098 Da

50.400 Ų

19

0

337.000

0

2

抑制剂

Rho- 相关蛋白激酶抑制剂