Home MAPK p38 MAPK inhibitor - Apoptosis related activator - Autophagy activator Losmapimod For research use only.

Losmapimod

Synonyms: GW856553X, GSK-AHAB

Losmapimod 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 Chemical Structure

Losmapimod Chemical Structure

CAS No. 585543-15-3

Purity & Quality Control

Losmapimod Related Products

Signaling Pathway

p38 MAPK Signaling Pathways

p38 MAPK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PBMC Function assay 1 h Inhibition of p38alpha-dependent TNFalpha production in human PBMC preincubated for 1 hr before LPS challenge by ELISA, IC50=0.1 μM 19772287
Click to View More Cell Line Experimental Data

Biological Activity

Description Losmapimod 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)
In vitro
In vitro

Losmapimod (GW856553X, GW856553, GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor.
Kinase Assay In vitro assay
Inhibition of p38α and p38β are determined by use of a ligand-displacement fluorescence polarization assay.
Cell Research Cell lines MB135 iDUX4 myoblasts
Concentrations 1 µM
Incubation Time 2 h
Method

Cells were treated with indicated concentration of drug for 2 h.
In Vivo
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]
Animal Research Animal Models Spontaneously hypertensive stroke-prone rats
Dosages ~12 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04264442 Active not recruiting
Facioscapulohumeral Muscular Dystrophy (FSHD)
Fulcrum Therapeutics
 February 13 2020 Phase 2
NCT04004000 Active not recruiting
Facioscapulohumeral Muscular Dystrophy 1
Fulcrum Therapeutics
 August 23 2019 Phase 2
NCT04003974 Completed
Facioscapulohumeral Muscular Dystrophy (FSHD)
Fulcrum Therapeutics
 August 9 2019 Phase 2
NCT02000440 Completed
Glomerulosclerosis Focal Segmental
GlaxoSmithKline
 July 1 2014 Phase 2

Chemical Information & Solubility

Molecular Weight 383.46 Formula

C22 H26 F N3 O2
CAS No. 585543-15-3 SDF Download Losmapimod SDF
Smiles CC1=C(C=C(C=C1F)C(=O)NC2CC2)C3=NC=C(C=C3)C(=O)NCC(C)(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 76 mg/mL ( (198.19 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 76 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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