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)

color 

White to off-white

Safety Information

HS Code 

2933399990

Losmapimod (GW856553X) Usage And Synthesis

Description

GW 856553X is a dual inhibitor of p38α and p38β MAPK (K_is = 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.

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