Chemical Property of Losmapimod (GW856553X)
Chemical Property:
- Boiling Point:529.37 °C at 760 mmHg
- PKA:7.75±0.46(Predicted)
- Flash Point:273.953 °C
- PSA：78.07000
- Density:1.21 g/cm3
- LogP:5.01380
- Solubility.:insoluble in EtOH; insoluble in H2O; ≥19.15 mg/mL in DMSO
- XLogP3:3.8
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:4
- Rotatable Bond Count:6
- Exact Mass:383.20090524
- Heavy Atom Count:28
- Complexity:573
- Purity/Quality:
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99%, *data from raw suppliers
Losmapimod *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CC1=C(C=C(C=C1F)C(=O)NC2CC2)C3=NC=C(C=C3)C(=O)NCC(C)(C)C
- Recent ClinicalTrials:Efficacy and Safety of Losmapimod in Treating Participants With Facioscapulohumeral Muscular Dystrophy (FSHD) (REACH)
- Recent EU Clinical Trials:A Phase 2, Randomized, Double-Blind, Placebo-Controlled, 24-Week, Parallel-Group Study of the Efficacy and Safety of Losmapimod in Treating Subjects with Facioscapulohumeral Muscular Dystrophy (FSHD)
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Description
GW 856553X is a dual inhibitor of p38α and p38β MAPK (Kis = 0.0079 and 0.025 μM, respectively, in cell-free assays). It is selective for p38α and p38β MAPK over p38γ and p38δ MAPK when used at a concentration of 10 μM. GW 856553X inhibits LPS-induced TNF-α production in isolated rat and human peripheral blood mononuclear cells (PBMCs; IC50s = 0.6 and 0.13 μM, respectively). It decreases disease severity in a mouse model of collagen-induced arthritis when administered at doses ranging from 0.8 to 20 mg/kg. GW 856553X (1.2 and 12 mg/kg) improves survival, normalizes blood pressure, and reduces increases in plasma levels of HDL, LDL, and triglycerides in spontaneously hypertensive stroke-prone rats fed a high-salt high-fat diet.
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Uses
Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor.
