SAR407899

SKU: orb1299861

Description

SAR407899 is a potent and selective Rho kinase (ROCK) inhibitor. It effectively blocks endothelin-1-induced vasoconstriction in renal resistance arteries, making it a valuable research tool for studying vascular tone, hypertension, and renal hemodynamics in both in vitro and in vivo models.

Research Area

Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 923359-38-0
• MW: 244.29
• Purity: 99.42% (May vary between batches)
• Formula: C₁₄H₁₆N₂O₂
• SMILES: O=c1[nH]ccc2cc(OC3CCNCC3)ccc12
• Target: Rho,ROCK
• Solubility: DMSO:6 mg/mL (24.56 mM)

Bioactivity

• Target IC50:
  ROCK2:102 nM (IC50)|ROCK1:276 nM (IC50)
• In Vivo:
  In vivo, SAR407899 dose-dependently induced rabbit penile erection, with greater potency and longer duration of action than sildenafil.
• Animal Research:
  Compared the effects of SAR407899, the Rho-kinase inhibitor Y-27632 and the PDE5 inhibitor sildenafil for their ability to relax corpus cavernosum strips contracted with phenylephrine in healthy and diabetic animals. Strips were obtained from WKY, spontaneous hypertensive (SHR), control CD, and diabetic CD rats, humans, control and diabetic rabbits. Diabetes was induced by streptozotocin or alloxan injection. In vivo penile erection (length) induced by drugs was measured in conscious rabbits.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, SAR407899, SAR-407899, SAR 407899, Rho-kinase, Rho, Rho-associated kinase, Rho-associated protein kinase, ROK, ROCK

Compound Identifiers

PubChem CID

15604510