Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BI-671800 (AP-761) 是高特异性的前列腺素 D2 受体拮抗剂,对哮喘有研究潜力,对人和小鼠 CRTH2 转染细胞中 PGD2 结合 CRTH2 的 IC50值分别为 4.5 和 3.7 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 928 | 现货 | ||
2 mg | ¥ 1,370 | 现货 | ||
5 mg | ¥ 2,130 | 现货 | ||
10 mg | ¥ 3,680 | 现货 | ||
25 mg | ¥ 5,950 | 现货 | ||
50 mg | ¥ 8,230 | 现货 | ||
100 mg | ¥ 10,900 | 现货 | ||
500 mg | ¥ 22,200 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,560 | 现货 |
产品描述 | BI-671800 (AP-761) is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2). With IC50 values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively. BI-671800 has the potential to treat poorly controlled asthma[2]. |
靶点活性 | CRTH2 (mouse):3.7 nM (in CRTH2 transfected cells), CRTH2 (human):4.5 nM (in CRTH2 transfected cells) |
体外活性 | BI-671800 (compound A) exhibits low nM potency as a potent small-molecule antagonist of human or mouse CRTH2 in transfected cells[1]. |
体内活性 | BI-671800 (compound A, 0.1-10 mg/kg, i.g.) shows significant inhibition of AHR in mice[1]. BI-671800 (compound A) also effectively blocks edema formation and greatly reduces the inflammatory infiltrate and skin pathology observed in drug vehicle-treated animals[3]. |
别名 | AP-761, Cmpd A |
分子量 | 501.5 |
分子式 | C25H26F3N5O3 |
CAS No. | 1093108-50-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 130 mg/mL (259.22 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.994 mL | 9.9701 mL | 19.9402 mL | 49.8504 mL |
5 mM | 0.3988 mL | 1.994 mL | 3.988 mL | 9.9701 mL | |
10 mM | 0.1994 mL | 0.997 mL | 1.994 mL | 4.985 mL | |
20 mM | 0.0997 mL | 0.4985 mL | 0.997 mL | 2.4925 mL | |
50 mM | 0.0399 mL | 0.1994 mL | 0.3988 mL | 0.997 mL | |
100 mM | 0.0199 mL | 0.0997 mL | 0.1994 mL | 0.4985 mL |
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。
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。
BI-671800 1093108-50-9 Endocrinology/Hormones GPCR/G Protein Immunology/Inflammation Prostaglandin Receptor GPR BI 671800 Inhibitor AP 761 inhibit BI671800 AP-761 AP761 Cmpd A inhibitor