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Ro-24-4736

产品编号 T16768 CAS 125030-71-9

Ro 24-4736 is an effective and selective platelet-activating factor antagonist.

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Ro-24-4736, CAS 125030-71-9

规格	价格/CNY	货期
25 mg	￥ 16,100	10-14周
50 mg	￥ 21,300	10-14周
100 mg	￥ 27,500	10-14周

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Ro 24-4736 is an effective and selective platelet-activating factor antagonist.
体外活性	Ro 24-4736 competes with [3H]PAF for its receptor site on dog platelets (IC50: 9.8±1.0 nM). Ro 24-4736 selectively inhibits PAF-induced aggregation of guinea pig, dog, and human platelets with concentration dependence [1].
体内活性	Ro 24-4736 is markedly superior in terms of p.o. potency, bioavailability, and p.o. duration of action in comparison with other PAF antagonists evaluated in this guinea pig model. Ro 24-4736 is a new platelet-activating factor antagonist. Ro 24-4736 displays no inhibitory activity toward the bronchoconstrictor effects of leukotriene D4 or histamine. Ro 24-4736 dose-dependently inhibits in vivo bronchoconstriction (ID50: 0.006-mg/kg p.o.) and ex vivo platelet aggregation (ID50: 0.004 mg/kg; p.o.) induced by PAF in guinea pigs. Time course studies display a complete blockade of PAF-induced platelet aggregation (ex vivo) up to 8 hr after a single p.o. the 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). 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. 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 indicates 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 [1][2].

分子量	546.04
分子式	C31H20ClN5OS
CAS No.	125030-71-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

计算器

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分子量计算器

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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.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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