Losmapimod

CAS No. 585543-15-3

Losmapimod( GSK-AHAB | GW856553X | SB856553 | GW 856553X | SB 856553 )

Catalog No. M15150 CAS No. 585543-15-3

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.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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2MG 27 In Stock
5MG 43 In Stock
10MG 64 In Stock
25MG 128 In Stock
50MG 213 In Stock
100MG 385 In Stock
500MG 872 In Stock
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Biological Information

  • Product Name
    Losmapimod
  • Note
    Research use only, not for human use.
  • Brief 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.
  • 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).
  • In Vitro
    ——
  • 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).
  • Synonyms
    GSK-AHAB | GW856553X | SB856553 | GW 856553X | SB 856553
  • Pathway
    MAPK/ERK Signaling
  • Target
    p38 MAPK
  • Recptor
    p38α|p38β
  • Research Area
    Cardiovascular Disease
  • Indication
    Ischemia

Chemical Information

  • CAS Number
    585543-15-3
  • Formula Weight
    383.4591
  • Molecular Formula
    C22H26FN3O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 58 mg/mL
  • SMILES
    O=C(C1=CC=C(C2=CC(C(NC3CC3)=O)=CC(F)=C2C)N=C1)NCC(C)(C)C
  • Chemical Name
    3-Pyridinecarboxamide, 6-[5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Willette RN, et al. J Pharmacol Exp Ther. 2009 Sep;330(3):964-70. 2. Cheriyan J, et al. Circulation. 2011 Feb 8;123(5):515-23. 3. Lomas DA, et al. J Clin Pharmacol. 2012 Mar;52(3):416-24.
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