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| | Losmapimod (GW856553X) Basic information |
| Product Name: | Losmapimod (GW856553X) | | Synonyms: | 6-[5-(Cyclopropylcarbamoyl)-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)pyridine-3-carboxamide;GW-856553;GSK-AHAB;GW 856553X;LosMapiMod;LosMapiMod,GW-856553;Losmapimod (GW856553X);3-Pyridinecarboxamide, 6-[5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)- | | CAS: | 585543-15-3 | | MF: | C22H26FN3O2 | | MW: | 383.46 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 585543-15-3.mol |  |
| | Losmapimod (GW856553X) Chemical Properties |
| 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) |
| | Losmapimod (GW856553X) Usage And Synthesis |
| 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. | | Definition | ChEBI: 6-[5-[(cyclopropylamino)-oxomethyl]-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)-3-pyridinecarboxamide is a phenylpyridine. | | target | p38α | | 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. |
| | Losmapimod (GW856553X) Preparation Products And Raw materials |
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