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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Cited by 1 Publication

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]
(Cell-free assay)		 p38β [1]
(Cell-free assay)
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

Animal Research:

[1]
+ Expand
  • Animal Models: Spontaneously hypertensive stroke-prone rats
  • Formulation: --
  • Dosages: ~12 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 76 mg/mL (198.19 mM)
Ethanol 41 mg/mL warmed (106.92 mM)
Water 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 9 2014 Phase 2
NCT00910962 Completed Acute Coronary Syndrome GlaxoSmithKline October 8 2009 Phase 2
NCT01218126 Completed Pulmonary Disease Chronic Obstructive GlaxoSmithKline November 4 2010 Phase 2
NCT02145468 Completed Acute Coronary Syndrome GlaxoSmithKline|The TIMI Study Group June 3 2014 Phase 3
NCT01648192 Completed Acute Coronary Syndrome GlaxoSmithKline July 24 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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p38 MAPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID