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Bosentan

Catalog #: 6232 Datasheet / COA / SDS
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6232/50
6232/10
Bosentan | CAS No. 147536-97-8 | Non-selective Endothelin Receptor Antagonists
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Description: High affinity dual ETA and ETB receptor antagonist;orally bioavailable
Alternative Names: Ro 47-0203

Chemical Name: 4-(1,1-Dimethylethyl)-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2'-bipyrimidin]-4-yl]benzenesulfonamide

Purity: ≥98%

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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

M.Wt:
551.61
Formula:
C27H29N5O6S
Solubility:
Soluble to 100 mM in DMSO and to 50 mM in ethanol
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
147536-97-8

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

  1. Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist.
    Clozel et al.
    J.Pharmacol.Exp.Ther., 1994;270:228
  2. 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
  3. 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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