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 4 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)
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PBMC M1jydmZ2dmO2aX;uJIF{e2G7 NYmyV5B5OSCq M1jlVWlvcGmkaYTpc44hd2ZicEO4ZYxxcGFvZHXw[Y5l\W62IGTOSoFteGijIIDyc4R2[3Srb36gbY4hcHWvYX6gVGJOSyCycnXpcoN2[mG2ZXSg[o9zKDFiaIKgZoVnd3KnIFzQV{BkcGGubHXu[4Uh[nliRVzJV2EtKEmFNUC9NE4yKM7:TR?= M3LlTlE6Pzd{Mki3

... Click to View More Cell Line Experimental Data
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]
- Collapse
  • 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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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p38 MAPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID