Application |
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A mixed endothelin receptor antagonist. Used as a vasodilator. Antihypertensive. |
Payment mode |
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Credit / Debit / Purchase Order |
Taxes |
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All prices are inclusive taxes |
Refund Policy |
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30 days money back guarantee |
References |
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"Clozel; M,; et al,: J, Pharmacol, Exp, Ther,; 270; 228 (1994); Gutsch; G,; et al,: Cardiovasc, Drugs Ther,; 10; 717 (1996); Weber; C,; et al,: Clin Pharmacol, Ther,; 60; 124 (1996); Krum; H,; et al,: N, Engl, J, Med,; 338; 784 (1998)" |
Canonical SMILES |
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CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)NC2=C(C(=NC(=N2)C3=NC=CC=N3)OCCO)OC4=CC=CC=C4OC
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Isomeric SMILES |
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CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)NC2=C(C(=NC(=N2)C3=NC=CC=N3)OCCO)OC4=CC=CC=C4OC |
InChI |
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InChI=1S/C27H29N5O6S/c1-27(2,3)18-10-12-19(13-11-18)39(34,35)32-23-22(38-21-9-6-5-8-20(21)36-4)26(37-17-16-33)31-25(30-23)24-28-14-7-15-29-24/h5-15,33H,16-17H2,1-4H3,(H,30,31,32) |
InchIKey |
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GJPICJJJRGTNOD-UHFFFAOYSA-N |
IUPAC Name |
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4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-ylpyrimidin-4-yl]benzenesulfonamide |
Exact Mass |
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551.18385484 |
Solubility |
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Poorly soluble in water (1.0 mg/100 ml) and in aqueous solutions at low pH (0.1 mg/100 ml at pH 1.1 and 4.0; 0.2 mg/100 ml at pH 5.0). Solubility increases at higher pH values (43 mg/100 ml at pH 7.5). |
Use Classification |
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Human drugs -> Tracleer -> EMA Drug Category |
Hazard Class |
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Acute Tox. 4 (50%) |
Description |
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Bosentan is a sulfonamide, a member of pyrimidines and a primary alcohol. It has a role as an antihypertensive agent and an endothelin receptor antagonist. |
EC Number |
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643-099-1 |
Toxicity Summary |
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Bosentan has been given as a single dose of up to 2400 mg in normal volunteers, or up to 2000 mg/day for 2 months in patients, without any major clinical consequences. The most common side effect was headache of mild to moderate intensity. In the cyclosporine A interaction study, in which doses of 500 and 1000 mg b.i.d. of bosentan were given concomitantly with cyclosporine A, trough plasma concentrations of bosentan increased 30-fold, resulting in severe headache, nausea, and vomiting, but no serious adverse events. Mild decreases in blood pressure and increases in heart rate were observed. There is no specific experience of overdosage with bosentan beyond the doses described above. Massive overdosage may result in pronounced hypotension requiring active cardiovascular support. |