Catalog No.S7215 Synonyms: GW856553, GSK-AHAB
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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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|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.|
|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). |
|In vitro||DMSO||76 mg/mL (198.19 mM)|
|Ethanol||41 mg/mL warmed (106.92 mM)|
* 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.
C22 H26 F N3 O2
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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|
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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