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Ro-24-4736

MCE 国际站：Ro-24-4736

品牌：MedChemExpress (MCE)

货号：HY-19097

CAS 号：125030-71-9

生物活性： Ro 24-4736 是一种强效、选择性强、作用持久的血小板活化因子 (PAF) 拮抗剂。Ro-24-4736 是一种点击化学试剂，含有炔基，可与含有叠氮基的分子发生铜催化叠氮-炔环加成反应 (CuAAc)。

体外研究(In Vitro)：Ro 24-4736 competes with [3H]PAF for its receptor site on dog platelets with an IC50 of 9.8±1.0 nM and selectively inhibits PAF-induced aggregation of guinea pig, dog and human platelets with concentration dependence[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)：Ro 24-4736 dose-dependently inhibits in vivo bronchoconstriction (ID50 of 0.006-mg/kg p.o.) and ex vivo platelet aggregation (ID50 of 0.004 mg/kg p.o.) induced by PAF in guinea pigs. Time course studies show complete blockade of PAF-induced platelet aggregation (ex vivo) up to 8 hr after a single p.o. dose of 0.03 mg/kg as well as a long duration of action in vivo (30 hr). The in vivo PAF antagonistic activity is specific because, even at high p.o. doses (up to 10 mg/kg), Ro 24-4736 shows no inhibitory activity toward the bronchoconstrictor effects of leukotriene D4 or histamine. In comparison with other PAF antagonists evaluated in this guinea pig model, Ro 24-4736 is markedly superior in terms of p.o. potency, bioavailability and p.o. duration of action. Studies are also performed with Ro 24-4736 in additional in vivo models. When administered p.o. to sensitized guinea pigs, the drug attenuates inhaled antigen-induced airway hyper-reactivity without effect on bronchoalveolar lavage leukocyte accumulation[1]. Ro 24-4736 is a new platelet activating factor antagonist. The tissue distribution of the 14C-label in male rats following a single intravenous dose of 1.0 mg/kg of 14C-Ro 24-4736 indicats appreciable uptake by the liver, kidney, heart and gastrointestinal tract. Peak plasma and tissue concentrations are seen at 5 minutes after dosing except for the small intestine (4 hrs) and abdominal fat, stomach and large intestine (4 hrs). At 48 hours, only 3.5% of the dose is present in the tissues, and 6.1% in the lumen of the gastrointestinal tracts[2]. MCE尚未独立确认这些方法的准确性。 仅供参考。

分子量：546.04

Formula：C31H20ClN5OS

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。

提供质量检测报告：Data Sheet、产品使用指南

产品活性：Ro 24-4736 是一种长效的选择性血小板活化因子 (PAF) 拮抗剂。

IC50 & Target：PAF[1]

相关产品：PAF (C18)  | Kadsurenone  | Foropafant  | Ginkgolide B  | Ginkgolide B (Standard)  | Lyso-PAF C-18  | Carbamyl-PAF  | 2-O-Ethyl PAF C-16  | TCV-309 chloride  | Hexanolamino PAF C-16  | Pyrrolidino PAF C-16  | rel-(2R,4R)-2,4-Bis(3,4,5-trimethoxyphenyl)-1,3-dioxolane

热门产品线：抑制剂  | 稳定性同位素标记物  |  脂质  |  糖类

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]. Crowley HJ, et al. Pharmacology of a potent platelet-activating factor antagonist: Ro 24-4736. J Pharmacol Exp Ther. 1991 Oct;259(1):78-85.
[2]. Anastasi EM, et al. Disposition and metabolism of Ro 24-4736 in the rat. Life Sci. 1994;54(26):PL483-90.