Bosentan Inhibitor CAS No. 147536-97-8

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KI1350	Bosentan	10 mg	$374
KI1350	Bosentan	50 mg	$1496

Chemical Characteristic

Product Name	Bosentan
Synonyms	Tracleer
CAS No.	147536-97-8
Molecular Weight	551.61
Formula	C₂₇H₂₉N₅O₆S
Chemical Name	Benzenesulfonamide, 4-(1,1-dimethylethyl)-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2'-bipyrimidin]-4-yl]-
Smiles	c1(ccc(cc1)C(C)(C)C)S(=O)(=O)Nc1nc(nc(c1Oc1c(cccc1)OC)OCCO)c1ncccn1
Chemical Structure

Biological activities

Bosentan is a dual endothelin receptor antagonist used in the treatment of pulmonary artery hypertension (PAH). Bosentan is a competitive antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors with IC50 values of 10 and 900 nM, respectively. Bosentan competitively antagonizes the specific binding of endothelin-1 on human smooth muscle cells (ET-A receptors) with a Ki value of 4.7 nM and on human placenta (ET-B receptors) with a Ki value of 95 nM.^[1] In the isolated perfused and ventilated rat lung (IPL), bosentan completely prevents the IRL1620-induced vasoconstriction with an IC50 of 3 µM.^[2] Pretreatment with bosentan (100 mg/kg/day) completely blocks the pulmonary vasoconstrictor response to acute hypoxia. Chronic bosentan treatment (100 mg/kg/day) instituted 48 hours before hypoxic exposure prevents the subsequent development of pulmonary hypertension, attenuates the associated right heart hypertrophy, and prevents the remodeling of small (50-100 microns) pulmonary arteries without altering systemic arterial pressure.^[3]

Protocols

In vivo: Bosentan is dissolved in distilled water.^[3]

References

[1] Clozel M, et al. Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist. J Pharmacol Exp Ther. 1994, 270(1): 228-235. [2] Martin C, et al. Differential effects of the mixed ET(A)/ET(B)-receptor antagonist bosentan on endothelin-induced bronchoconstriction, vasoconstriction and prostacyclin release. Naunyn Schmiedebergs Arch Pharmacol. 2000, 362(2): 128-136. [3] Chen SJ, et al. Endothelin-receptor antagonist bosentan prevents and reverses hypoxic pulmonary hypertension in rats. J Appl Physiol. 1995, 79(6): 2122-2131.

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