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编 号:F615933
分子式:C17H19N3O3S
分子量:345.42
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
BMS 182874 is an orallyactive, highly selective endothelin receptor (ETA receptor) antagonist, with IC50 value of 0.150 μM, Ki of 0.055 μM. BMS 182874 reduces the arterial pressure of Deoxycorticosterone acetate (HY-B1472) induced hypertension model in rats, and can be used for cardiovascular disease research.

体内研究:
BMS 182874 (100 μM/kg;单次口服) 使动脉血压从对照水平缓慢下降 25%。给药 12 和 24 小时后,动脉血压仍比对照水平低 12%。Animal Model:Kidney Deoxycorticosterone acetate -salt hypertensive rats
Dosage:100 μM/kg
Administration:Oral gavage (p.o.); Intravenous injection (i.v.)
Result:Made arterial pressure slowly fell by 25% from a control level. After dosing for 12 and 24 h, makes arterial pressure is still 12% below the control level.

体外研究:
BMS-182874 (dimethyla minoanalogue 11) 是 ETA 诱导的细胞内 Ca2+ 增加的有效的功能拮抗剂,在 vsm -A10 细胞中的 IC50 值为 0.150 μM, Ki 值为 0.055 μM,在兔颈动脉环中 KB 值为 0.520 μM。
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