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Seratrodast
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Seratrodast图片
CAS NO:112665-43-7
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
25mg电议
50mg电议

产品介绍
Seratrodast(AA 2414) 是一种抗哮喘药,也是一种有效的选择性血栓素 A2 受体 (TP) 拮抗剂。
Cas No.112665-43-7
别名塞曲司特; AA 2414
化学名ζ-(2,4,5-trimethyl-3,6-dioxo-1,4-cyclohexadien-1-yl)-benzeneheptanoic acid
Canonical SMILESOC(CCCCCC(C1=CC=CC=C1)C(C(C(C)=C2C)=O)=C(C)C2=O)=O
分子式C22H26O4
分子量354.4
溶解度≥ 10.9mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 7.4 nM for guinea pig platelets

Seratrodast is a thromboxane A2 (TXA2) receptor antagonist.

Thromboxane A2, a type of thromboxane, is produced by activated platelets and has prothrombotic properties, such as stimulating activation of new platelets and increasing platelet aggregation.

In vitro: Seratrodast was found to inhibit the aggregation of guinea pig platelets induced by a prostaglandin endoperoxide analogue, U-44069 and the specific binding of another analogue, [3H]U-46619 to washed guinea pig platelets. Seratrodast could competitively inhibit the contraction of rabbit aorta and pig coronary arteries induced by U-44069. Seratrodast also inhibited the contraction of rabbit aorta induced by PGF2 alpha and the contraction of pig coronary arteries. However, seratrodast had no effect on the antiaggregatory effect of guinea pig platelets [1].

In vivo: In experiments with guinea pigs, oral seratrodast at 0.1-1 mg/kg could dose-dependently inhibit the platelet aggregation induced by U-44069; the inhibition at 1 mg/kg was 100% at 1 hr and was 89% even at 24 hr after seratrodast administration [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Imura, Y. ,Terashita, Z.,Shibouta, Y., et al. Antagonistic action of AA-2414 on thromboxane A2/prostaglandin endoperoxide receptor in platelets and blood vessels. Japanese Journal of Pharmacology 52(1), 35-53 (1990).