Sitaxsentan sodium (TBC-11251) is a selective endothelin receptor-A antagonist with IC50 and Ki value of 1.4 nM and 0.43 nM, respectively. Sitaxsentan sodium inhibits ET-1-induced stimulation of phosphoinositide turnover with a Ki of 0.69 nM and a pA2 of 8.0. Sitaxsentan blocks the action of endothelin (ET) on the endothelin-A (ETA) receptor selectively (by a factor of 6000 compared to the ETB). Sitaxsentan blocked increased plasma endothelin levels in the prevention protocol but did not affect the established elevated levels in the intervention study.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 40 mg/mL|
Selective endothelin A receptor antagonism with sitaxsentan for pulmonary arterial hypertension associated with connective tissue disease.
Girgis RE, et al. Ann Rheum Dis. 2007 Nov;66(11):1467-72. PMID: 17472992.
STRIDE 1: effects of the selective ET(A) receptor antagonist, sitaxsentan sodium, in a patient population with pulmonary arterial hypertension that meets traditional inclusion criteria of previous pulmonary arterial hypertension trials.
Langleben D, et al. J Cardiovasc Pharmacol. 2004 Nov;44 Suppl 1:S80-4. PMID: 15838366.
Attenuation of pulmonary vascular hypertension and cardiac hypertrophy with sitaxsentan sodium, an orally active ET(A) receptor antagonist.
Tilton RG, et al. Pulm Pharmacol Ther. 2000;13(2):87-97. PMID: 10799286.
|Related Endothelin Receptor Products|
Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM.
Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.
Bosentan is an endothelin (ET) receptors antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.
Macitentan is an orally-active, tissue-targeting dual ET receptor antagonist.
Ambrisentan is an orally active, highly selective antagonist of the endothelin-1 type A receptor.
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