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Chemical Structure : ML221
CAS No.: 877636-42-5
Catalog No.: PC-63277Not For Human Use, Lab Use Only.
ML221 is a potent, selective, functional antagonist of apelin receptor (APJ) with IC50 of 1.75 uM in the β-arrestin assay, >37-fold selective over the closely related AT1 receptor.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $198 | In stock | |
| 50 mg | $298 | In stock | |
| 100 mg | $498 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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ML221 is a potent, selective, functional antagonist of apelin receptor (APJ) with IC50 of 1.75 uM in the β-arrestin assay, >37-fold selective over the closely related AT1 receptor.
ML221 inhibits apelin-13-mediated activation of APJ in cAMP assays with IC50 of 0.7 uM.
ML221 inhibits cholangiocarcinoma proliferation and angiogenesis, significantly decreases tumor growth in nu/nu mice.
| M.Wt | 385.35 | |
| Formula | C17H11N3O6S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
|
| Chemical Name/SMILES |
5-[(4-Nitrobenzoyl)oxy]-2-[(2-pyrimidinylthio)methyl]-4H-pyran-4-one |
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1. Maloney PR, et al. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6656-60.
2. Sakamoto K, et al. Eur J Pharmacol. 2016 Nov 15;791:213-220.
3. Ishimaru Y, et al. Sci Rep. 2017 Nov 8;7(1):15062.
4. Hall C, et al. Cancer Lett. 2017 Feb 1;386:179-188.
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