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- 5-HT Receptor
- (4E)-SUN9221
(4E)-SUN9221
(4E)-SUN9221是一种有效的α1-adrenergicreceptor和5-HT2receptor拮抗剂，具有抗高血压和抗血小板聚集的功效。
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包装价格促销价数量
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1mg￥15250.0012200.00- +
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5mg￥34325.0027460.00- +
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10mg￥58387.0046710.00- +
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20mg￥103012.0082410.00- +
- 货号: ajce49530
- CAS: 222318-55-0
- 别名:
- 分子式: C25H31FN4O3
- 分子量: 454.54
- 纯度: ＞98%
- 溶解度: Soluble in DMSO
- 储存: Store at -20°C
- 库存: 现货
Background
(4E)-SUN9221 is a potent antagonist of α1-adrenergic receptor and 5-HT2 receptor, with antihypertensive and anti-platelet aggregation activities.
(4E)-SUN9221 potently inhibits collagen-, ADP- and epinephrine-induced platelet aggregation, with IC50s of 10 nM, 35 nM, 14 nM, respectively, in human platelet-rich plasma (PRP). (4E)-SUN9221 displays potent α1-adrenergic antagonist activity (pA2 =8.89±0.21) and 5-HT2 antagonist activity (pA2 =8.74±0.22)[1].
(4E)-SUN9221 (1, 3, 10 mg/kg, p.o.) reduces the blood pressure in a dose-dependent manner in conscious spontaneously hypertensive rats (SHR). (4E)-SUN9221 (3 mg/kg) exhibits antihypertensive activity in SHR[1].
[1]. Mizuno A, et al. Synthesis and pharmacological evaluation of pyrroloazepine derivatives as potent antihypertensive agents with antiplatelet aggregation activity. Chem Pharm Bull (Tokyo). 1999 Feb;47(2):246-56.
