Losmapimod (GW856553X)

Catalog No.S7215 Synonyms: GW856553, GSK-AHAB

For research use only.

Losmapimod (GW856553X, GW856553, GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. P38 MAPKs are involved in cell differentiation, apoptosis and autophagy. Phase 3.

Losmapimod (GW856553X) Chemical Structure

CAS No. 585543-15-3

Selleck's Losmapimod (GW856553X) has been cited by 13 publications

Purity & Quality Control

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Biological Activity

Description Losmapimod (GW856553X, GW856553, GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. P38 MAPKs are involved in cell differentiation, apoptosis and autophagy. 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 NYiwcHlrTnWwY4Tpc44h[XO|YYm= Mlz5NUBp M4S3Z2lvcGmkaYTpc44hd2ZicEO4ZYxxcGFvZHXw[Y5l\W62IGTOSoFteGijIIDyc4R2[3Srb36gbY4hcHWvYX6gVGJOSyCycnXpcoN2[mG2ZXSg[o9zKDFiaIKgZoVnd3KnIFzQV{BkcGGubHXu[4Uh[nliRVzJV2EtKEmFNUC9NE4yKM7:TR?= Mln2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5N{KyPFcoRjF7N{eyNlg4RC:jPh?=
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 (from reference)

Animal Research:

[1]

  • Animal Models: Spontaneously hypertensive stroke-prone rats
  • Dosages: ~12 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 383.46
Formula

C22 H26 F N3 O2

CAS No. 585543-15-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C=C(C=C1F)C(=O)NC2CC2)C3=NC=C(C=C3)C(=O)NCC(C)(C)C

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04264442 Enrolling by invitation Drug: Losmapimod Facioscapulohumeral Muscular Dystrophy (FSHD) Fulcrum Therapeutics February 13 2020 Phase 2
NCT04004000 Active not recruiting Drug: Losmapimod Facioscapulohumeral Muscular Dystrophy 1 Fulcrum Therapeutics August 23 2019 Phase 2
NCT04003974 Completed 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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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.

Handling Instructions

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