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| 化学名: | ボセンタン一水和物 | | 英語化学名: | Bosentan hydrate | | 别名: | Bosetan;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;Bosentan Hydrate
See B675900;Benzenesulfonamide, 4-(1,1-dimethylethyl)-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2'-bipyrimidin]-4-yl]-, hydrate (1:1);Bosentan (200 mg);bosentan hydrate;Bosentan monohydrate | | CAS番号: | 157212-55-0 | | 分子式: | C27H31N5O7S | | 分子量: | 569.62934 | | EINECS: | 1592732-453-0 | | カテゴリ情報: | Inhibitors;API;Heterocyclic Compounds | | Mol File: | 157212-55-0.mol |  |
| 融点 | 114-118 °C | | 貯蔵温度 | 2-8°C | | 溶解性 | DMSO (Slightly), Methanol (Very Slightly, Heated) | | 外見 | powder | | 色 | white to beige | | Merck | 14,1353 |
| | ボセンタン一水和物 Usage And Synthesis |
| 外観 | 白色～うすい黄色, 結晶～粉末 | | 溶解性 | エタノールに溶ける。 | | 用途 | エンドセリン受容体（ETA 及
びETB）拮抗作用を示します。 | | 用途 | エンドセリン受容体（ETA及 びETB）の拮抗作用を示します。肺高血圧を 改善します。 | | 効能 | 血圧降下薬, エンドセリン受容体拮抗薬 | | 商品名 | トラクリア (アクテリオンファーマシューティカルズジャパン); トラクリア (アクテリオンファーマシューティカルズジャパン) | | 使用 | Antagonist
(endothelin receptor). | | 使用 | Bosentan hydrate has been used in cell viability assay. It has also been used as a positive control for calcium transient analysis. | | 定義 | ChEBI: Bosentan hydrate is a hydrate. It contains a bosentan. | | brand name | Tracleer (Actelion). | | 生物活性 | a sulfonamide-derived, competitive and specific endothelin receptor antagonist with a relatively higher affinity to the endothelin a receptor than endothelin b receptor. by competitively binding to endothelin a and endothelin b receptors in the endothelium and vascular smooth muscle, bosentan offset the effect of endothelin which is an extremely potent endogenous vasoconstrictor and broncho-constrictor. in addition, bosentan decreases both pulmonary and systemic vascular resistance and is particularly applied in the treatment of pulmonary arterial hypertension. [1] | | Biochem/physiol Actions | Bosentan is an endothelin receptor antagonist. Endothelin is a potent vasoconstrictor, making antagonists of clinical interest for the treatment of conditions associated with vasospasm, such as subarachnoid hemorrhage (SAH) and hypertension. Bosentan is a dual endothelin receptor antagonist effective in the treatment of pulmonary arterial hypertension (PAH), the first of the class to make it to market. Bosentan is an orally available, competitive antagonist of both the ETA and ETB receptor subtypes with a Ki of 4.7 nM for ETA and a Ki of 95 nM for ETB. | | in vitro | a study was performed in vitro to measure the influence of bosentan on the angiogenic performance of dermal microvascular endothelial cells (mvecs) and to detect the capacity of bosentan in offsetting the antiangiogenic effects of systemic sclerosis sera. it was found that bosentan significantly increased cell viability and offset the antiangiogenic effects of systemic sclerosis sera on dermal mvecs. [2] | | in vivo | a study was conducted to investigate the effect of bosentan on plasma leptin level after myocardial infarction in wistar rats. after oral administration of bosentan once daily at the dose of 100 mg/kg for 2 days, concentration of leptin in plasma significantly increased. this finding revealed that bosentan played an crucial role on regulating leptin concentration in ischemic cardiovascular pathology. [1] | | IC 50 | inhibiting endothelin receptor a and b with an ic50 of 15.1 ± 1.6 μm in p388/dx cells. | | 参考文献 | [1] ostrowski rp, januszewski sa, kowalska za and kapuscinski a. effect of endothelin receptor antagonist bosentan on plasma leptin concentration in acute myocardial infarction in rats. pathophysiology. 2003 sep; 9(4): 249-56.
[2]romano e, bellando-randone s, manetti m, bruni c, lepri g, matucci-cerinic m, guiducci s. bosentan blocks the antiangiogenic effects of sera from systemic sclerosis patients: an in vitro study. clin exp rheumatol. 2015 aug; 33(4 suppl 91): s148-52.
[3]rubin lj, badesch db, barst rj, galiè n, black cm et, al. bosentan therapy for pulmonary arterial hypertension. new engl j med. 2002 mar; 346 (12): 896-903. |
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