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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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) 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] p38β [1]
8.1(pKi) 7.6(pKi)
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

Solubility (25°C)

In vitro DMSO 76 mg/mL (198.19 mM)
Ethanol 41 mg/mL warmed (106.92 mM)
Water <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or 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 Conditions Sponsor/Collaborators Start Date Phases
NCT02299375 Completed Pulmonary Disease, Chronic Obstructive GlaxoSmithKline December 2014 Phase 2
NCT02000440 Completed Glomerulosclerosis, Focal Segmental GlaxoSmithKline July 2014 Phase 2
NCT02145468 Completed Acute Coronary Syndrome GlaxoSmithKline|The TIMI Study Group June 2014 Phase 3
NCT01756495 Completed Acute Coronary Syndrome GlaxoSmithKline January 2013 Phase 1
NCT01648192 Completed Acute Coronary Syndrome GlaxoSmithKline July 2012 Phase 1
NCT01541852 Completed Chronic Obstructive Pulmonary Disease Cambridge University Hospitals NHS Foundation Trust|Technology Strategy Board, United Kingdom|GlaxoSmithKline|Royal Brompton & Harefield NHS Foundation Trust|University of Cambridge June 2012 Phase 2

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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