ML221 |
| カタログ番号GC14855 |
ML 221 は強力なアペリン (APJ) 機能的アンタゴニストであり、アペリン 13 を介した APJ の活性化を阻害します。IC50 は cAMP アッセイで 0.70 μM、β-アレスチン アッセイで 1.75 μM、EC80 は両方のアッセイで 10 nM です。 .
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Cas No.: 877636-42-5
Sample solution is provided at 25 µL, 10mM.
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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 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/
References:
[1]. Maloney PR, et al. Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6656-60.
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