Losmapimod (GW856553X)

Catalog No.S7215 Synonyms: GW856553, GSK-AHAB

Losmapimod (GW856553X) Chemical Structure

Molecular Weight(MW): 383.46

Losmapimod (GW856553X) is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. Phase 3.

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Cited by 3 Publications

1 Customer Review

  • Intracellular pathways of b-adrenoceptor-induced proliferation. Urothelial proliferation (% of basal responses) in T24 in the absence and presence of (d) losmapimod (1-30 μM).

    Auton Autacoid Pharmacol, 2015, 35(3):32-40.. Losmapimod (GW856553X) purchased from Selleck.

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Biological Activity

Description Losmapimod (GW856553X) is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. Phase 3.
Targets
p38α [1]
(Cell-free assay)		 p38β [1]
(Cell-free assay)
8.1(pKi) 7.6(pKi)
In vivo In spontaneously hypertensive stroke-prone rats (SHR-SP), Losmapimod significantly improves survival, endothelial-dependent and -independent vascular relaxation, and indices of renal function, and subsequently attenuates dyslipidemia, hypertension, cardiac remodeling, plasma renin activity (PRA), aldosterone, and interleukin-1beta (IL-1beta). [1]

Protocol

Animal Research:

[1]
+ Expand
  • Animal Models: Spontaneously hypertensive stroke-prone rats
  • Formulation: --
  • Dosages: ~12 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 76 mg/mL (198.19 mM)
Ethanol 41 mg/mL warmed (106.92 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 383.46
Formula

C22 H26 F N3 O2
CAS No. 585543-15-3
Storage powder
in solvent
Synonyms GW856553, GSK-AHAB

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04004000 Recruiting Drug: Losmapimod Facioscapulohumeral Muscular Dystrophy 1 Fulcrum Therapeutics August 23 2019 Phase 2
NCT04003974 Recruiting Drug: Losmapimod|Drug: Placebo oral tablet Facioscapulohumeral Muscular Dystrophy (FSHD) Fulcrum Therapeutics August 9 2019 Phase 2
NCT02000440 Completed Drug: Losmapimod Glomerulosclerosis Focal Segmental GlaxoSmithKline July 1 2014 Phase 2
NCT00976560 Completed Drug: GW856553|Other: Placebo Depressive Disorder Major GlaxoSmithKline September 25 2009 Phase 2

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p38 MAPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID