Losmapimod (GW856553X)

For research use only.

Catalog No.S7215 Synonyms: GW856553, GSK-AHAB

11 publications

Losmapimod (GW856553X) Chemical Structure

CAS No. 585543-15-3

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.

Selleck's Losmapimod (GW856553X) has been cited by 11 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.

Purity & Quality Control

Choose Selective p38 MAPK Inhibitors

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 Mme4SpVv[3Srb36gZZN{[Xl? M{DHelEhcA>? MojqTY5pcWKrdHnvckBw\iCyM{jhcJBp[S2mZYDlcoRmdnRiVF7GZYxxcGFicILv[JVkfGmxbjDpckBpfW2jbjDQRm1EKHC{ZXnuZ5Vj[XSnZDDmc5IhOSCqcjDi[YZwemViTGDTJINp[WyuZX7n[UBjgSCHTFnTRUwhUUN3ME2wMlEh|ryP MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTd5MkK4O{c,OTl5N{KyPFc9N2F-

... 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
  • Dosages: ~12 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

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

* 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
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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Mass Concentration Volume Molecular Weight

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

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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p38 MAPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID