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180384-57-0

中文名稱 TEZOSENTAN
英文名稱 TEZOSENTAN
CAS 180384-57-0
分子式 C27H27N9O6S
分子量 605.62
MOL 文件 180384-57-0.mol
180384-57-0 結(jié)構(gòu)式 180384-57-0 結(jié)構(gòu)式

基本信息

中文別名
化合物 T17064
英文別名
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

物理化學(xué)性質(zhì)

熔點(diǎn)198-200°
沸點(diǎn)761.2±70.0 °C(Predicted)
密度1.432±0.06 g/cm3(Predicted)
儲(chǔ)存條件Sealed in dry,2-8°C
溶解度Soluble in DMSO
酸度系數(shù)(pKa)2.93±0.10(Predicted)
形態(tài)Solid
顏色Off-white to gray

常見(jiàn)問(wèn)題列表

生物活性
Tezosentan (RO 610612) 是內(nèi)皮素 (ET) 受體的一個(gè)拮抗劑,其對(duì) ETA 和 ETB 受體的 pA2 值分別為 9.5,7.7。
靶點(diǎn)

ET A

9.5 (pA2)

ET B

7.7 (pA2)

體外研究

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%.

體內(nèi)研究

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.

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