Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BAY-1797 是具有口服活性的选择性P2X4高效拮抗剂,对人 P2X4 的IC50为 211 nM,具有抗伤害和抗炎作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 348 | 现货 | ||
5 mg | ¥ 813 | 现货 | ||
10 mg | ¥ 1,490 | 现货 | ||
25 mg | ¥ 3,230 | 现货 | ||
50 mg | ¥ 4,770 | 现货 | ||
100 mg | ¥ 6,780 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 913 | 现货 |
产品描述 | BAY-1797 is an orally active and selective P2X4 antagonist (IC50: 211 nM against human P2X4) with anti-nociceptive and anti-inflammatory effects. BAY-1797 displays no or very weak activity on the other P2X ion channels. |
靶点活性 | human P2X7:10.6 μM , human P2X4:211 nM , human P2X23:>30 μM , human P2X1:>50 μM , human P2X3:8.3 μM |
体外活性 | BAY-1797 inhibits human, mouse, and rat P2X4 in 1321N1 cells (IC50s: 108 nM, 112 nM, and 233 nM). BAY-1797 exerts no measurable activity on hERG and carbonic anhydrase II (both IC50>10 μM). BAY-1797 (10 μM) is also tested against a panel of off-targets, including GPCRs, ion channels, kinases, and transporters. Inhibitory activity against the dopamine transporter (IC50: 2.17 μM) was revealed as the only hit. |
体内活性 | BAY-1797 (12.5-50 mg/kg; p.o.) shows a significant induction of PGE2 levels in the inflamed paw in the mouse Complete Freund’s Adjuvant (CFA) inflammatory pain model. BAY-1797 (50 mg/kg; once daily for multiple p.o.) induces a significant reduction of the ipsilateral paw load 24 and 48 h after CFA injection. BAY-1797 treatment shows the AUCnorm, Vss, and t1/2 are 1.06 kg h/L, 3.67 L/kg, and 2.64 hours, respectively. |
分子量 | 416.88 |
分子式 | C20H17ClN2O4S |
CAS No. | 2055602-83-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 250 mg/mL (599.69 mM), sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3988 mL | 11.9939 mL | 23.9877 mL | 59.9693 mL |
5 mM | 0.4798 mL | 2.3988 mL | 4.7975 mL | 11.9939 mL | |
10 mM | 0.2399 mL | 1.1994 mL | 2.3988 mL | 5.9969 mL | |
20 mM | 0.1199 mL | 0.5997 mL | 1.1994 mL | 2.9985 mL | |
50 mM | 0.048 mL | 0.2399 mL | 0.4798 mL | 1.1994 mL | |
100 mM | 0.024 mL | 0.1199 mL | 0.2399 mL | 0.5997 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。
BAY-1797 2055602-83-8 Membrane transporter/Ion channel Neuroscience P2X Receptor paw ion inhibit anti-inflammatory CFA Complete BAY1797 P2XRs Freund’s selective channel BAY 1797 inflamed Inhibitor Adjuvant P2X anti-nociceptive inhibitor