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ML221
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ML221图片
CAS NO:877636-42-5
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
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。
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)

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.

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>

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.

Cas No.

877636-42-5

分子式

C17H11N3O6S

分子量

385.35

储存和溶解度

DMSO:3.9 mg/mL(10 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years