Powder: -20°C for 3 years | In solvent: -80°C for 2 years
A-987306 是一种高效、口服生物可利用的组胺H4拮抗剂,对大鼠和人 H4作用的Ki 值分别为 3.4 nM 和 5.8 nM。 A-987306 在小鼠腹膜炎模型中显示出抗炎活性。
产品描述 | A-987306 is a potent and oral bioavailable histamine H 4 antagonist, with Kis of 3.4 nM and 5.8 nM for rat H4, and human H4. A-987306 exhibits anti-inflammatory activity in mice peritonitis model [1]. |
体外活性 | A-987306 is a potent and functional antagonist in vitro of human, rat, and mouse H4 receptors in cell-based FLIPR assays [1]. A-987306 is 620-fold, >1600-fold, and 162-fold selective for the human H 4 R over the human H 1, H 2, and H 3 receptors in cell-based Ca 2+ -flux functional assay (FLIPR) [1]. A-987306 shows lower selectivity for H 4 R in the rat (only 4-fold selective for the rat H 4 R over the rat H 3 R) in FLIPR [1]. |
体内活性 | A-987306 (98.23 μg/kg-9.82 mg/kg; i.p.) has been shown to reduce scratching induced by the histamine H 4 agonist clobenpropit [1]. A-987306 (10 mg/kg; p.o.) has a moderate fractional oral bioavailability (F po/iv =26%) with a half-life of 3.7 h and a C max of 0.30 μM at a T max of 1.5 h after dosing [1]. Animal Model: Mice [1] Dosage: 98.23 μg/kg, 327.42 μg/kg, 982.26 μg/kg, 9.82 mg/kg (Pharmacokinetic Analysis) Administration: Intraperitoneal injection Result: F po/iv =26%, T 1/2 =3.7 hours, C max =0.30 μM, T max =1.5 hours |
分子量 | 327.432 |
分子式 | C18H25N5O |
CAS No. | 1082954-71-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
( < 1 mg/mL refers to the product slightly soluble or insoluble )
对于不同动物的给药剂量换算,您也可以参考 更多...
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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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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