Ambrisentan 177036-94-1

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Ambrisentan

Molecular Weight: 378.42 Ambrisentan, a highly selective antagonist of the endothelin-1 type A receptor with IC50 of 18 nM, is indicated for the treatment of pulmonary arterial hypertension (PAH).


Biological Activity


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)	378.42
Formula	C22H22N2O4
CAS No.	177036-94-1

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	LU-208075,BSF-208075

Solubility (25°C) *	In vitro	DMSO	76 mg/mL (200.83 mM)
		Water	<1 mg/mL (
		Ethanol	22 mg/mL (58.13 mM)

Chemical Name	(αS)-α-[(4,6-dimethyl-2-pyrimidinyl)oxy]-β-methoxy-β-phenyl-benzenepropanoic acid

Stock Solution (1ml DMSO)	1mM	10mM	20mM	30mM
Mass(mg)	0.37842	3.7842	7.5684	11.3526

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