Bosentan
Chemical Name: 4-(1,1-Dimethylethyl)-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2'-bipyrimidin]-4-yl]benzenesulfonamide
Purity: ≥98%
Biological Activity
Bosentan is a high affinity dual ETA and ETB receptor antagonist (Ki values are 4.7 and 95 nM for ETA and ETB, respectively). Inhibits ET-1 induced contraction of isolated rat aorta and sarafotoxin S6C-induced contraction of rat trachea in vitro. Orally bioavailable.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist.
Clozel et al.
J.Pharmacol.Exp.Ther., 1994;270:228 -
Effects of bos. (Ro 47-0203), an ETA-, ETB-receptor antagonist, on regional haemodynamic responses to endothelins in conscious rats.
Gardiner et al.
Br.J.Pharmacol., 1994;112:823 -
Human pluripotent stem cells identify molecular targets of trisomy 12 in chronic lymphocytic leukemia patients
JC Reid, D Golubeva, AL Boyd, CG Hollands, C Henly, L Orlando, A Leber, J Hébert, F Morabito, G Cutrona, L Agnelli, M Gentile, M Ferrarini, A Neri, B Leber, M Bhatia
Cell Reports, 2021;34(11):108845.
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