Losmapimod

SKU: orb1224583

Description

Losmapimod (GSK-AHAB, GW856553X, SB856553) is a selective, potent, orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively; displays no significant activity for p38γ, p38δ (<25% inhibition at 10 uM), and COX-2; significantly and dose-dependently improves survival, endothelial-dependent and -independent vascular relaxation in rat model of cardiovascular disease.Ischemia Phase 3 Clinical(In Vitro):In the spontaneously hypertensive stroke-prone rat (SHR-SP), chronic treatment with GSK-AHAB significantly and dose-dependently improves survival, endothelial-dependent and -independent vascular relaxation, and indices of renal function, and it attenuates dyslipidemia, hypertension, cardiac remodeling, plasma renin activity (PRA), aldosterone, and interleukin-1β (IL-1β).

Key Properties

• CAS Number: 585543-15-3
• MW: 383.4591
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₆FN₃O₂
• SMILES: O=C(C1=CC=C(C2=CC(C(NC3CC3)=O)=CC(F)=C2C)N=C1)NCC(C)(C)C
• Target: p38 MAPK
• Solubility: DMSO: ≥ 58 mg/mL

Bioactivity

• In Vivo:
  In the spontaneously hypertensive stroke-prone rat (SHR-SP), chronic treatment with GSK-AHAB significantly and dose-dependently improves survival, endothelial-dependent and-independent vascular relaxation, and indices of renal function, and it attenuates dyslipidemia, hypertension, cardiac remodeling, plasma renin activity (PRA), aldosterone, and interleukin-1β (IL-1β).

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

GSK-AHAB | GW856553X | SB856553 | GW 856553X | SB 856553

Quick Database Links

Gene Symbol

p38 MAPK