SAR-407899

SAR-407899 Property

storage temp. Store at -20°C
solubility H2O : 50 mg/mL (178.09 mM; Need ultrasonic)DMSO : 25 mg/mL (89.05 mM; Need ultrasonic)
form Powder
color Light yellow to khaki
FDA UNII AD9C9XVB9T

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal wordWarning
Hazard statements H315-H319-H335
Precautionary statements P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P362-P403+P233-P501

SAR-407899 Chemical Properties,Usage,Production

Uses SAR407899 hydrochloride is a selective, potent and ATP-competitive ROCK inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively.
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^[1]. 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^[2].
IC 50 ROCK-2: 102 nM (IC₅₀); ROCK-1: 276 nM (IC₅₀)
References [1] L?hn M, et al. Pharmacological characterization of SAR407899, a novel rho-kinase inhibitor. Hypertension. 2009 Sep;54(3):676-83. DOI:10.1161/HYPERTENSIONAHA.109.134353
[2] Guagnini F, et al. Erectile properties of the Rho-kinase inhibitor SAR407899 in diabetic animals and human isolated corpora cavernosa. J Transl Med. 2012 Mar 23;10:59. DOI:10.1186/1479-5876-10-59
[3] Chen W, et al. Screening RhoA/ROCK inhibitors for the ability to prevent chronic rejection of mouse cardiac allografts.Transpl Immunol. 2018 Jun 6. pii: S0966-3274(18)30029-7. DOI:10.1016/j.trim.2018.06.002

SAR-407899 Preparation Products And Raw materials

Raw materials

Preparation Products

SAR-407899 Suppliers

Global(71)Suppliers

SAR-407899 Spectrum

API
抑制剂
生物化工
细胞生物学试剂
ROCK激酶抑制剂(SAR407899 HYDROCHLORIDE)
6-(哌啶-4-氧基)异喹啉-1(2H)-酮盐酸盐,10 MM DMSO 溶液
6-(哌啶-4-基氧基)异喹啉-1(2H)-酮盐酸盐
6-(哌啶-4-氧基)异喹啉-1(2H)-酮盐酸盐
6-(4-哌啶基氧基)-1(2H)-异喹啉酮盐酸盐
923262-96-8
SAR407899 hydrochloride, 10 mM in DMSO
SAR-407899,Rho-associated protein kinase,ROK,Rho-associated kinase,SAR 407899,SAR-407899 hydrochloride,Rho-kinase,Inhibitor,inhibit,SAR407899 hydrochloride,ROCK,SAR407899
SAR 407899;SAR407899
SAR-407899 （SAR407899，SAR 407899）
CS-2364
6-(4-Piperidinyloxy)-1(2H)-isoquinolinone hydrochloride (1:1)
6-(4-Piperidinyloxy)-1(2H)-isoquinolinone hydrochloride
SAR407899 HCl
SAR407899 (hydrochloride)
6-(piperidin-4-yloxy)isoquinolin-1(2h)-one hcl
6-(piperidin-4-yloxy)isoquinolin-1(2H)-one hydrochloride
SAR-407899
SAR407899
SAR 407899