KD025

SKU: orb1221664

Description

SLx-2119, also known as KD-025, is an orally bioavailable inhibitor of ROCK-II that is greater than 200-fold selective over ROCK-I (IC50s = 105 nM and 24 μM, respectively).(In Vitro):Belumosudil (SLx-2119; 40 μM) induces significant down-regulations of Tsp-1 and CTGF mRNA levels in PASMC. The microarray hybridized with aRNA from HMVEC treated with Belumosudil, shows a 5-times higher background than the other arrays.(In Vivo):Belumosudil (KD-025; 100, 200 or 300 mg/kg, i.p.) dose-dependently reduces infarct volume after transient middle cerebral artery occlusion. Belumosudil is at least as efficacious in aged, diabetic or female mice, as in normal adult males.

Key Properties

• CAS Number: 911417-87-3
• MW: 452.51
• Purity: >98% (HPLC)
• Formula: C₂₆H₂₄N₆O₂
• SMILES: C(=O)(COc1cc(ccc1)c1nc2c(c(n1)Nc1cc3cn[nH]c3cc1)cccc2)NC(C)C
• Target: ROCK2| ROCK2
• Solubility: DMSO : ≥ 29 mg/mL; 64.09 mM

Bioactivity

• In Vivo:
  Belumosudil (KD-025; 100, 200 or 300 mg/kg, i.p.) dose-dependently reduces infarct volume after transient middle cerebral artery occlusion. Belumosudil is at least as efficacious in aged, diabetic or female mice, as in normal adult males.
  Read more...
• In Vitro:
  Belumosudil (SLx-2119; 40 μM) induces significant down-regulations of Tsp-1 and CTGF mRNA levels in PASMC. The microarray hybridized with aRNA from HMVEC treated with Belumosudil, shows a 5-times higher background than the other arrays.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SLx-2119 | SLx2119 | SLx 2119 | KD 025

Quick Database Links

Gene Symbol

ROCK2| ROCK2