Bosentan

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Cat.No. 6232 - Bosentan | C27H29N5O6S | CAS No. 147536-97-8
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)
Datasheet
Citations
Literature

Biological Activity

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
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 551.61. Batch specific molecular weights may vary from batch to batch due to solvent 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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Product Datasheets

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References

References are publications that support the products' biological activity.

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 bosentan (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, supplier, High, affinity, endothelin, antagonists, antagonism, ETA, ETB, orally, bioavailable, Ro470203, Ro, 47-0203, Non-selective, Endothelin, Tocris Bioscience

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Pathways for Bosentan

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