- SAR-407899
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- $1.00
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2020-03-16
- CAS:923262-96-8
- Min. Order: 1KG
- Purity: 97%-99.9%
- Supply Ability: 100KG
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| | SAR-407899 Basic information |
| Product Name: | SAR-407899 | | Synonyms: | SAR-407899;6-(piperidin-4-yloxy)isoquinolin-1(2H)-one hydrochloride;6-(piperidin-4-yloxy)isoquinolin-1(2h)-one hcl;SAR407899 (hydrochloride);SAR407899 HCl;6-(4-Piperidinyloxy)-1(2H)-isoquinolinone hydrochloride;6-(4-Piperidinyloxy)-1(2H)-isoquinolinone hydrochloride (1:1);CS-2364 | | CAS: | 923262-96-8 | | MF: | C14H17ClN2O2 | | MW: | 280.74998 | | EINECS: | | | Product Categories: | API | | Mol File: | 923262-96-8.mol |  |
| | SAR-407899 Chemical Properties |
| 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 |
| | SAR-407899 Usage And Synthesis |
| 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) | | References | [1] Lhn 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 |
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