ML221
Cat. No.:YN480241
产品名称: | ML221 |
CAS No.: | 877636-42-5 |
Chemical Name: | 5-[(4-nitrobenzoyl)oxy]-2-[(2-pyrimidinylthio)methyl]-4H-pyran-4-one |
Synonyms: | ML221; ML 221; ML-221 |
分子量: | 385.35 |
分子式: | C₁₇H₁₁N₃O₆S |
SMILES: | O=C1C=C(CSC2=NC=CC=N2)OC=C1OC(C3=CC=C([N+]([O-])=O)C=C3)=O |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | ML221 是一种apelin (APJ)拮抗剂,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。 |
IC50和靶点: | |
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Maloney, P.R., Khan, P., Hedrick, M., 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) receptorBioorg. Med. Chem. Lett.22(21),6656-6660(2012)
Hall, C., Ehrlich, L., Venter, J., et al.Inhibition of the apelin/apelin receptor axis decreases cholangiocarcinoma growthCancer Lett.386,179-188(2017)
Xiong, Q., He, W., Wang, H., et al.Effect of the spinal apelin‑APJ system on the pathogenesis of chronic constriction injury‑induced neuropathic pain in ratsMol. Med. Rep.16(2),1223-1231(2017)
Ishimaru, Y., Shibagaki, F., Yamamuro, A., et al.An apelin receptor antagonist prevents pathological retinal angiogenesis with ischemic retinopathy in miceSci. Rep.7(1),15062(2017)