| Identification | Back Directory | [Name]
SAR407899 | [CAS]
923359-38-0 | [Synonyms]
SAR407899 free base
6-(piperidin-4-yloxy)isoquinolin-1(2H)-one
-6-(piperidin-4-yloxy)-2H-isoquinolin-1-one
1(2H)-Isoquinolinone, 6-(4-piperidinyloxy)- | [Molecular Formula]
C14H16N2O2 | [MOL File]
923359-38-0.mol | [Molecular Weight]
244.29 |
| Chemical Properties | Back Directory | [Boiling point ]
517.8±50.0 °C(Predicted) | [density ]
1.193±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 6 mg/mL (24.56 mM; Need warming) | [form ]
Powder | [pka]
12.79±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
SAR407899 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. SAR407899 shows stable inhibition of migrasome formation. | [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] Puzhong Lu, et al. Chemical screening identifies ROCK1 as a regulator of migrasome formation. Cell Discov. 2020 Aug 4;6(1):51. DOI:10.1038/s41421-020-0179-6 |
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| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
|