Bosentan (200 mg)
Bosentan monohydrate
CAS: 157212-55-0
Molecular Formula: C27H31N5O7S
Bosentan (200 mg) - Names and Identifiers
| Name | Bosentan monohydrate |
| Synonyms | CS-170 Bosetan Bosentan hydrate bosentan hydrate Bosentan (200 mg) Bosentan monohydrate Bosentan Hydrate See B675900 4-(tert-Butyl)-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-[2,2'-bipyrimidin]-4-yl)benzenesulfona 4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-Methoxyphenoxy)-2-(pyriMidin-2-yl)pyriMidin-4-yl]benzene-1-sulfonaMide 4-(1,1-Dimethylethyl)-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)(2,2'-bipyrimidin)-4-yl)benzenesulfonamide monohydrate |
| CAS | 157212-55-0 |
| EINECS | 1592732-453-0 |
| InChI | InChI=1/C27H29N5O6S.H2O/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);1H2 |
Bosentan (200 mg) - Physico-chemical Properties
| Molecular Formula | C27H31N5O7S |
| Molar Mass | 569.62934 |
| Melting Point | 114-118 °C |
| Boling Point | 742.3°C at 760 mmHg |
| Flash Point | 402.8°C |
| Solubility | DMSO 113 mg/mL Water 0.001 mg/mL Ethanol 2 mg/mL |
| Vapor Presure | 3.84E-23mmHg at 25°C |
| Appearance | powder |
| Color | white to beige |
| Merck | 14,1353 |
| Storage Condition | 2-8°C |
| In vitro study | Bosentan competitive antagonism [. |
| In vivo study | Both intravenous and oral Bosentan inhibited the pressor response by more than ET-1, with long duration of activity and no intrinsic agonist activity. Bosentan can also inhibit the buck and boost effects of ET-1 and sarafotoxin S6C. The pharmacological properties make Bosentan a potential drug for clinical vasoconstriction-related diseases. Bosentan was the first orally available non-polypeptide mixed ETA/B receptor antagonist. Long-term treatment with Bosentan in rats with congestive heart failure (CHF) significantly improved survival, Hemodynamics and cardiac remodeling. Bosentan can reduce arterial blood pressure with an effect comparable to that of angiotensin-converting enzyme (ACE) inhibitors. Bosentan-treated CHF rats after acute myocardial infarction can reduce arterial blood pressure and have an additive effect on ACE inhibitors. Acute or chronic treatment with Bosentan can improve systemic and Pulmonary hemodynamics in patients with CHF by reducing peripheral and pulmonary vascular resistance and increasing cardiac output. |
Bosentan (200 mg) - Risk and Safety
| HS Code | 2935909550 |
Bosentan (200 mg) - Reference
| Reference Show more | 1. Bai Yiping, Feng Jianguo, Liu Li et al.. Effect of endothelin A receptor antagonist pretreatment on renal function after extracorporeal circulation in dogs [J]. Chongqing Medical 2018 047(010):1305-1308 1313. 2. [IF = 5.923] Qiao Zhang et al."Salvianolic Acid A, as a Novel ETA Receptor Antagonist, Shows Inhibitory Effects on Tumor in Vitro." Int J Mol Sci. 2016 Aug;17(8):1244 |
Bosentan (200 mg) - Reference Information
| biological activity | Bosentan (Ro 47-0203) is an endothelin (ET) receptor antagonist with targets of ET-A and ET-B,Ki is 4.7 nM and 95 nM respectively. |
| target | TargetValue ET-A 4.7 nM(Ki) ET-B 95 nM(Ki) |
| Target | Value |
| ET-A | 4.7 nM(Ki) |
| ET-B | 95 nM(Ki) |
| in vitro studies | Bosentan competitive antagonism [. |
| in vivo studies | intravenous injection and oral Bosentan can inhibit the pressor reaction caused by large ET-1, with long activity time and no inherent agonist activity. Bosentan can also suppress the buck and boost effects of ET-1 and sarafotoxin S6C. Pharmacological properties make Bosentan a potential drug for clinical vasoconstriction-related diseases. Bosentan is the first non-polypeptide mixed ETA/B receptor antagonist that can be taken orally. Long-term treatment with Bosentan for rats with congestive heart failure (CHF) can significantly improve survival rate, hemodynamics and cardiac remodeling. Bosentan can reduce arterial blood pressure, and the effect is equivalent to that of angiotensin converting enzyme (ACE) inhibitors. Bosentan-treated CHF rats after acute myocardial infarction can reduce arterial blood pressure and have additive effect on ACE inhibitors. Bosentan acute or chronic treatment can improve the systemic and pulmonary hemodynamics of CHF patients by reducing peripheral vascular and pulmonary vascular resistance and increasing cardiac output. |
| use | endothelin receptor antagonist; treatment of pulmonary hypertension |
Last Update：2024-04-09 21:04:16
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