Bosentan

Name: Bosentan
Brand: Tocris Bioscience
SKU: 6232

Tocris Bioscience, part of Bio-Techne | Catalog # 6232

Citations (6)

COA / SDS

High affinity dual ETA and ETB receptor antagonist;orally bioavailable

Key Product Details

Description:	High affinity dual ET_A and ET_B 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)
Molecular Weight:	551.61

View Full Technical Details for Bosentan

Technical Data
Citations

Biological Activity for Bosentan

Bosentan is a high affinity dual ET_A and ET_B receptor antagonist (K_i values are 4.7 and 95 nM for ET_A and ET_B, 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 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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References for Bosentan

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

Gardiner Effects of bos. (Ro 47-0203), an ET_A-, ET_B-receptor antagonist, on regional haemodynamic responses to endothelins in conscious rats. Br.J.Pharmacol. 1994 PMID: 7921608
Clozel Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist. J.Pharmacol.Exp.Ther. 1994 PMID: 8035319