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ML221

Cat. No.:YN480241

  • CAS No. :877636-42-5

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    • 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.
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      Purity: 98%
    • 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)

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