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YM158 free base

MCE 国际站：YM158 free base

品牌：MedChemExpress (MCE)

货号：HY-U00355

CAS 号：179102-65-9

生物活性： YM158 游离碱是一种强效且选择性的 LTD4 和 TXA2 受体拮抗剂，其 pA2 值分别约为 8.87 和 8.81。

体外研究(In Vitro)：YM158 antagonizes leukotriene (LT) D4 and thromboxane (TX) A2 receptors. Functional assays in vitro show that YM158 exhibits competitive dual antagonism of LTD4 and TXA2 receptor-mediated contraction of isolated guinea pig tracheae, with pA2 values of about 8.87 and 8.81, respectively. Its antagonistic activity for the LTD4 receptor is approximately 6.5 times less potent than that of Montelukast, and that for the TXA2 receptor is 2.5 times more potent than that of Seratrodast. YM158 also inhibits PGD2- and PGF2α -induced tracheal contractions. YM158 antagonizes the stable TXA2 analog U46619-induced aggregation of both guinea pig and human platelets and inhibits the LTD4-induced contraction of guinea pig ileum. YM158 produces a concentration-dependent inhibition of guinea pig ileum contraction induced by 1 nM LTD4 with an IC50 value of 0.58 nM[1]. MCE尚未独立确认这些方法的准确性。 仅供参考。

体内研究(In Vivo)：YM158, an orally active dual antagonist for LTD4 and TXA2 receptors, is expected to have a stronger antiasthmatic efficacy in a broader class of asthmatic patients than single antagonistic drugs.The effect of YM158 is examined on these asthmatic responses in mediator-controlled and passively sensitized guinea pigs. Because the inhibitory effects of YM158 on increase in the airway resistance induced by LTD4 or U46619 are shown to be dose-dependent when p.o. administered 1 h before LTD4 or U46619 injection, with ED50 values of 8.6 and 14 mg/kg, respectively, the antagonistic activities of p.o. YM158 for LTD4 and TXA2 receptors are exhibited at the same dose range. Oral YM158 shows significant effects, approximately the same as the combination of Pranlukast and Daltroban on antigen-induced response under various conditions; namely, where LTD4 is predominant, TXA2 is predominant; or where both mediators participated equally. In groups not treated with Indomethacin, administration of Daltroban (10 mg/kg), a combination of Pranlukast (30 mg/kg) and Daltroban (10 mg/kg), or YM158 (30 mg/kg) significantly prolongs the onset time for asthmatic response and significantly suppresses symptoms[2]. MCE尚未独立确认这些方法的准确性。 仅供参考。

分子量：681.22

Formula：C32H33ClN6O5S2

运输条件：美国大陆地区的室温；其他地区可能有所不同。

储存方式：请按照分析证书中推荐的条件储存产品。

Animal Administration [2]：Guinea pigs[2] Male Hartley guinea pigs are used. Effects of YM158 (30 mg/kg, p.o.) , Pranlukast, and Daltroban are measured on the shortening of onset time for asthmatic response. Each compound is administered p.o. to animals without or with 5 mg/kg or 1 mg/kg of Indomethacin[2]. MCE尚未独立确认这些方法的准确性。 仅供参考。

提供质量检测报告：Data Sheet、产品使用指南

产品活性：YM158 free base 是一种有效的选择性 LTD4 和 TXA2 受体拮抗剂, pA2 值分别为 8.87 和 8.81。

IC50 & Target：LTD4 8.87 (pA2)

相关产品：Quinotolast sodium  | MK-571  | MK-571 sodium  | Pranlukast  | Pranlukast (Standard)  | Desloratadine  | KP496  | Verlukast  | ONO4057  | Tryptanthrin  | Pranlukast hemihydrate  | Tryptanthrin (Standard)

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Trending products：Inhibitors  | Isotope-Labeled Compounds  |  Lipids  |  Saccharides

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客户发表文献：
[1]. Nature. 2026 Sep;657(8131):549-558.
[2]. Nature. 2026 Sep;657(8132):755-764.
[3]. Nature. 2026 Sep;657(8133):1027-1034.
[4]. Nature. 2026 Sep;657(8131):477-486.
[5].Nature. 2026 Sep;657(8132):789-799.
[6]. Nature. 2026 Sep;657(8131):517-524.
[7]. Nature. 2026 Sep;657(8133):1045-1052.
[8]. Cell. 2026 Sep 14:S0092-8674(26)01003-2.
[9]. Cell. 2026 Sep 3;189(18):5688-5705.e13.
[10]. Cell. 2026 Sep 2:S0092-8674(26)00937-2.

参考文献：
[1]. Arakida Y, et al. In vitro pharmacologic profile of YM158, a new dual antagonist for LTD4 and TXA2 receptors. J Pharmacol Exp Ther. 1998 Nov;287(2):633-9.
[2]. Arakida Y, et al. Effects of lipid mediator antagonists on predominant mediator-controlled asthmatic reactions in passively sensitized guinea pigs. J Pharmacol Exp Ther. 1999 Sep;290(3):1285-91.