Losmapimod (GW856553X) 585543-15-3

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Molecular Weight:

383.46 Losmapimod (GW856553X) is a selective, potent, and orally active p38 MAPK Inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. Phase 3.


Biological Activity

Description	Losmapimod (GW856553X) is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. Phase 3.
Targets	p38α [1]	p38β [1]
IC50	8.1(pKi)	7.6(pKi)
In vitro
In vivo	In spontaneously hypertensive stroke-prone rats (SHR-SP), Losmapimod significantly improves survival, endothelial-dependent and -independent vascular relaxation, and indices of renal function, and subsequently attenuates dyslipidemia, hypertension, cardiac remodeling, plasma renin activity (PRA), aldosterone, and interleukin-1beta (IL-1beta).
Features

Protocol(Only for Reference)


Kinase Assay: [1]

In vitro assay	Inhibition of p38α and p38β are determined by use of a ligand-displacement fluorescence polarization assay.

Animal Study: [1]

Animal Models	Spontaneously hypertensive stroke-prone rats
Formulation
Dosages	~12 mg/kg
Administration	p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	383.46
Formula	C22 H26 F N3 O2
CAS No.	585543-15-3

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	GW856553, GSK-AHAB

Solubility (25°C) *	In vitro	DMSO	76 mg/mL (198.19 mM)
		Water	<1 mg/mL (
		Ethanol	41 mg/mL heating (106.92 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	3-Pyridinecarboxamide, 6-[5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)-

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Product Categories : MAPK > p38 MAPK Inhibitor