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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。
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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 | 库存 | 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 | 5日内发货 | |
1 mL x 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是一种强效的apelin/APJ功能拮抗剂,能够抑制apelin-13介导的APJ激活,其在cAMP实验中的IC50为0.70 μM,在β-arrestin实验中的IC50为1.75 μM,且在两种实验中EC80均为10 nM。ML221对于与之密切相关的血管紧张素II型1(AT1)受体的选择性>37倍(IC50,>79 μM),且在细胞中显示出来。ML221对一系列GPCR表现出有限的交叉反应性,除了κ-阿片类受体和苯二氮卓受体(<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 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | DMSO: 6.25 mg/mL (16.219 mM), Sonication is recommended. | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
DMSO
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