- SAR407899
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- $50.00 / 5mg
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2025-11-10
- CAS:923359-38-0
- Min. Order:
- Purity: 99.42%
- Supply Ability: 10g
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| | 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 | | EINECS: | | | Product Categories: | | | 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 |
| | SAR407899 Preparation Products And Raw materials |
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