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Losmapimod (GW856553X)

Name: Losmapimod (GW856553X)
Brand: Selleck Chemicals
SKU: S7215
Rating: 5 (11 reviews)

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 pK_i 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 11 Publications

1 Customer Review

Purity & Quality Control

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p38 MAPK Signaling Pathway Map

Biological Activity

Description

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	MX\GeY5kfGmxbjDhd5NigQ>?		M4Lvb\|EhcA>?		NYC1RYs2UW6qaXLpeIlwdiCxZjDwN\|hidHCqYT3k[ZBmdmSnboSgWG5H[WyyaHGgdJJw\HWldHnvckBqdiCqdX3hckBRSk2FIIDy[Ylv[3WkYYTl[EBnd3JiMTDodkBj\W[xcnWgUHBUKGOqYXzs[Y5o\SCkeTDFUGlUSSxiSVO1NF0xNjFizszN	NVfxTHE6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3O\|IzQDdpPkG5O\|czOjh5PD;hQi=>

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 (from reference)

Animal Research: ^[1]	Animal Models: Spontaneously hypertensive stroke-prone rats Dosages: ~12 mg/kg Administration: p.o.

References

[1] Willette RN, et al. J Pharmacol Exp Ther. 2009, 330(3), 964-970.

Solubility (25°C)

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

Chemical Information

Molecular Weight	383.46
Formula	C₂₂ H₂₆ F N₃ O₂
CAS No.	585543-15-3
Storage	3 years	-20°C	powder
Storage	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

Download Losmapimod (GW856553X) SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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% DMSO + % + % Tween 80 + % ddH₂O

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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.

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

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 2022-01-17)

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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