Losmapimod (GW856553X)

Base Information

• Chemical Name: Losmapimod (GW856553X)
• CAS No.: 585543-15-3
• Deprecated CAS: 1201684-97-0
• Molecular Formula: C22H26FN3O2
• Molecular Weight: 383.46
• Hs Code.: 2933399990
• European Community (EC) Number: 629-887-8
• UNII: F2DQF16BXE
• ChEMBL ID: CHEMBL1088752
• DSSTox Substance ID: DTXSID30974109
• Metabolomics Workbench ID: 153289
• NCI Thesaurus Code: C96532
• Pharos Ligand ID: 633P5PGTY5YM
• Wikidata: Q6683687
• Wikipedia: Losmapimod
• Mol file: 585543-15-3.mol

Synonyms:GW856553X;

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:

98%, ^*data from raw suppliers

Losmapimod ^*data from reagent suppliers

Safty Information:

• Pictogram(s):  
• Hazard Codes: 

MSDS Files:

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)
• 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.
• Uses: Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor.