| Identification | Back Directory | [Name]
SAR-407899 | [CAS]
923262-96-8 | [Synonyms]
CS-2364
SAR407899
SAR-407899
SAR 407899
SAR407899 HCl
SAR 407899;SAR407899
SAR407899 (hydrochloride)
SAR-407899 （SAR407899，SAR 407899）
6-(piperidin-4-yloxy)isoquinolin-1(2h)-one hcl
6-(4-Piperidinyloxy)-1(2H)-isoquinolinone hydrochloride
6-(piperidin-4-yloxy)isoquinolin-1(2H)-one hydrochloride
6-(4-Piperidinyloxy)-1(2H)-isoquinolinone hydrochloride (1:1) | [Molecular Formula]
C14H17ClN2O2 | [MDL Number]
MFCD20485429 | [MOL File]
923262-96-8.mol | [Molecular Weight]
280.75 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 MYPTT696 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) | [storage]
Store at -20°C | [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 |
|
| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
|