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Submit ReviewBosentan
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 |
| InChI Key | GJPICJJJRGTNOD-UHFFFAOYSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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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Product Datasheets for Bosentan
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
If you know of a relevant reference for Bosentan, please let us know.
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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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