SAR407899
SAR407899 Basic information
- Product Name:
- SAR407899
- Synonyms:
-
- 6-(piperidin-4-yloxy)isoquinolin-1(2H)-one
- -6-(piperidin-4-yloxy)-2H-isoquinolin-1-one
- SAR407899 free base
- 1(2H)-Isoquinolinone, 6-(4-piperidinyloxy)-
- SAR 407899,Rho-associated kinase,ROK,Rho-kinase,ROCK,Rho-associated protein kinase,SAR407899,inhibit,SAR-407899,Inhibitor
- SAR407899, 10 mM in DMSO
- CAS:
- 923359-38-0
- MF:
- C14H16N2O2
- MW:
- 244.29
- Mol File:
- 923359-38-0.mol
SAR407899 Chemical Properties
- 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
SAR407899 Usage And Synthesis
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)
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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