Losmapimod (GW856553X)
- CAS NO.:585543-15-3
- Empirical Formula: C22H26FN3O2
- Molecular Weight: 383.46
- MDL number: MFCD16619322
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-08 20:21:46
What is Losmapimod (GW856553X)?
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.
The Uses of Losmapimod (GW856553X)
Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor.
What are the applications of Application
Losmapimod is a selective and potent p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively
Definition
ChEBI: 6-[5-[(cyclopropylamino)-oxomethyl]-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)-3-pyridinecarboxamide is a phenylpyridine.
References
[1]. willette rn, eybye me, olzinski ar, et al. differential effects of p38 mitogen-activated protein kinase and cyclooxygenase 2 inhibitors in a model of cardiovascular disease. j pharmacol exp ther, 2009, 330(3): 964-970.
[2]. cheriyan j, webb aj, sarov-blat l, et al. inhibition of p38 mitogen-activated protein kinase improves nitric oxide-mediated vasodilatation and reduces inflammation in hypercholesterolemia. circulation., 2011, 123(5): 515-523.
[3]. lomas da, lipson da, miller be, et al. an oral inhibitor of p38 map kinase reduces plasma fibrinogen in patients with chronic obstructive pulmonary disease. j clin pharmacol, 2012, 52(3): 416-424.
Properties of Losmapimod (GW856553X)
Boiling point: | 529.4±50.0 °C(Predicted) |
Density | 1.20±0.1 g/cm3(Predicted) |
storage temp. | Store at -20°C |
solubility | insoluble in EtOH; insoluble in H2O; ≥19.15 mg/mL in DMSO |
form | solid |
pka | 7.75±0.46(Predicted) |
color | White to off-white |
Safety information for Losmapimod (GW856553X)
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for Losmapimod (GW856553X)
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