Losmapimod (GW856553X)

Catalog No.S7215

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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Losmapimod (GW856553X) Chemical Structure

Losmapimod (GW856553X) Chemical Structure
Molecular Weight: 383.46

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

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]
IC50 8.1(pKi) 7.6(pKi)
In vitro
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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

In vitro assay Inhibition of p38α and p38β are determined by use of a ligand-displacement fluorescence polarization assay.

Animal Study: [1]

Animal Models Spontaneously hypertensive stroke-prone rats
Formulation
Dosages ~12 mg/kg
Administration p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

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

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-23)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02299375 Recruiting 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

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Chemical Information

Download Losmapimod (GW856553X) SDF
Molecular Weight (MW) 383.46
Formula

C22 H26 F N3 O2

CAS No. 585543-15-3
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms GW856553, GSK-AHAB
Solubility (25°C) * In vitro DMSO 76 mg/mL (198.19 mM)
Ethanol 41 mg/mL warming (106.92 mM)
Water <1 mg/mL (<1 mM)
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 Name 3-Pyridinecarboxamide, 6-[5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)-

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.

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