TEZOSENTAN
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- CAS号:
- 180384-57-0
- 英文名:
- TEZOSENTAN
- 英文别名:
- RO 610612;TEZOSENTAN;N-(2-(2-(2H-Tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl;N-(2-(2-(2H-Tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl)-5;N-(2-(2-(2H-Tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl)-5-isopropylpyridine-2-sulfonamide;N-[6-(2-Hydroxyethoxy)-5-(2-Methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)-4-pyridinyl]-4-pyriMidinyl]-5-(1-Methylethyl)-2-pyridinesulfonaMide;2-Pyridinesulfonamide, N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)-4-pyridinyl]-4-pyrimidinyl]-5-(1-methylethyl)-
- 中文名:
- TEZOSENTAN
- 中文别名:
- 化合物 T17064
- CBNumber:
- CB6790143
- 分子式:
- C27H27N9O6S
- 分子量:
- 605.62
- MOL File:
- 180384-57-0.mol
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TEZOSENTAN化学性质
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熔点:
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198-200°
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沸点:
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761.2±70.0 °C(Predicted)
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密度:
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1.432±0.06 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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2.93±0.10(Predicted)
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形态:
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Solid
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颜色:
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Off-white to gray
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TEZOSENTAN性质、用途与生产工艺
Tezosentan (RO 610612) 是内皮素 (ET) 受体的一个拮抗剂，其对 ETA 和 ETB 受体的 pA2 值分别为 9.5,7.7。
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ET
A
9.5 (pA2)
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ET
B
7.7 (pA2)
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Affinity of Tezosentan for the ET receptors is assessed in different cells and tissues. Tezosentan inhibits the specific
125
I-labeled ET-1 binding to ETA receptors with an inhibitory potency (K
i
) of 0.3 nM on CHO cells and of 18 nM on membranes of baculovirus-infected insect cells. Similarly, Tezosentan inhibits the specific binding of
125
I-labeled ET-1, ET-3, or sarafotoxin S6c to ET
B
receptors with an inhibitory affinity of 10 to 21 nM. Tezosentan up to a concentration of 1 μM did not exhibit any binding inhibitory activity in 27 radioligand binding assays different from ET binding. On H1 central, 5-hydroxytryptamine2A, and vasopressin V1 receptors, Tezosentan (1 μM) induces a weak inhibition of less than 20%.
In pithed Wistar rats, Tezosentan dose-dependently inhibits the pressor effect of big ET-1 (P<0.001 at all doses). At the lowest dose tested of 1 mg/kg, Tezosentan inhibits the pressor effect of the various doses of big ET-1 by 50 to 80%. Tezosentan has no effect by itself on blood pressure in these pithed rats. Tezosentan is very effective in a rat model of acute renal failure. ET antagonists have been shown to prevent the vasoconstriction and the renal failure that follow acute renal ischemia in rats.
TEZOSENTAN
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-17351 | Tezosentan | | 1 mg | 3820元 |
| 2024/04/30 | HY-17351 | Tezosentan | | 5 mg | 9550元 |
180384-57-0, TEZOSENTAN 相关搜索:
- Sulfur & Selenium Compounds
- Pharmaceuticals
- Intermediates & Fine Chemicals
- Heterocycles
- Aromatics
- C27H27N9O6S
- 化合物 T17064
- 180384-57-0
- 2-Pyridinesulfonamide, N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)-4-pyridinyl]-4-pyrimidinyl]-5-(1-methylethyl)-
- RO 610612
- N-(2-(2-(2H-Tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl)-5-isopropylpyridine-2-sulfonamide
- N-(2-(2-(2H-Tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl
- N-(2-(2-(2H-Tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl)-5
- N-[6-(2-Hydroxyethoxy)-5-(2-Methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)-4-pyridinyl]-4-pyriMidinyl]-5-(1-Methylethyl)-2-pyridinesulfonaMide
- TEZOSENTAN