Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ML221 是apelin (APJ)拮抗剂,能够抑制 apelin-13 介导的 APJ 的活化,在 cAMP 试验和 β-arrestin 实验中,IC50值分别为 0.70 μM 和 1.75 μM,EC80值均为 10 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 218 | 现货 | ||
5 mg | ¥ 485 | 现货 | ||
10 mg | ¥ 727 | 现货 | ||
25 mg | ¥ 1,280 | 现货 | ||
50 mg | ¥ 1,980 | 现货 | ||
100 mg | ¥ 3,520 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 533 | 现货 |
产品描述 | ML221 is a potent apelin /APJ functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays. |
靶点活性 | APJ:1.75 μM |
体外活性 | ML221 is a potent apelin/APJ functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays. ML221 is >37-fold selective over the closely related angiotensin II type 1 (AT1) receptor (IC50, >79 μM) in cells. ML221 displays limited cross reactivity against a range of GPCRs except the κ-opioid and benzodiazepinone receptors (<50/<70%I at 10 μM) |
细胞实验 | ML221 is dissolved in DMSO. Cells (angiotensin II receptor-like 1 (AGTRL-1) cell line) are seeded at 1000 cell/well (1536 plate) in 4 μL and grown overnight (16-18 h) at 37°C, 5% CO2, 100% humidity, then 60 nL of either DMSO control or 2 mM stock test compounds (ML221, etc.) in DMSO are transferred to each well, followed by 2 μL of 30 nM Apelin-13 to negative control and test compound wells, and 2 μL of assay media (F12 nutrient mix HAMs supplemented with 10% hi-FBS, 1× penicillin/streptomycin) to positive control wells. This yields a final concentration of test compound (ML221, etc.) of 20 μM and 1% final DMSO. Assay is incubated for 90 min at room temperature, and then developed with 3 μL of detection reagent for 60 min and luminescence read on a ViewLux. They are for reference only. |
分子量 | 385.35 |
分子式 | C17H11N3O6S |
CAS No. | 877636-42-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 3.9 mg/mL(10 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.595 mL | 12.9752 mL | 25.9504 mL | 64.8761 mL |
5 mM | 0.519 mL | 2.595 mL | 5.1901 mL | 12.9752 mL | |
10 mM | 0.2595 mL | 1.2975 mL | 2.595 mL | 6.4876 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。
ML221 877636-42-5 GPCR/G Protein Apelin receptor Arrestin inhibit ML-221 Inhibitor ML 221 inhibitor