Pricing Availability   Qty
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% (HPLC)

Biological Activity for Bosentan

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.

Compound Libraries for Bosentan

Bosentan is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for Bosentan

M. Wt 551.61
Formula C27H29N5O6S
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 147536-97-8
PubChem ID 104865
Smiles COC1=C(C=CC=C1)OC2=C(N=C(C3=NC=CC=N3)N=C2NS(=O)(C4=CC=C(C(C)(C)C)C=C4)=O)OCCO

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.

Solubility Data for Bosentan

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 55.16 100
ethanol 27.58 50

Preparing Stock Solutions for Bosentan

The following data is based on the product molecular weight 551.61. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.81 mL 9.06 mL 18.13 mL
5 mM 0.36 mL 1.81 mL 3.63 mL
10 mM 0.18 mL 0.91 mL 1.81 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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References for Bosentan

References are publications that support the biological activity of the product.

Clozel et al (1994) Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist. J.Pharmacol.Exp.Ther. 270 228 PMID: 8035319

Gardiner et al (1994) Effects of bos. (Ro 47-0203), an ETA-, ETB-receptor antagonist, on regional haemodynamic responses to endothelins in conscious rats. Br.J.Pharmacol. 112 823 PMID: 7921608

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Keywords: Bosentan, Bosentan supplier, High, affinity, endothelin, antagonists, antagonism, ETA, ETB, orally, bioavailable, Ro470203, Ro, 47-0203, Non-selective, Endothelin, 6232, Tocris Bioscience

Citations for Bosentan

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