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MK-0752

Cat. No.:YN380037

  • CAS No. :471905-41-6

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    • 参考文献
    • 产品名称: MK-0752
      CAS No.: 471905-41-6
      Chemical Name: cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)-cyclohexanepropanoic acid
      Synonyms:MK-0752,MK 0752
      分子量:442.90
      分子式:C₂₁H₂₁ClF₂O₄S
      SMILES:O=S([C@@]1(C2=C(C=CC(F)=C2)F)CC[C@@H](CCC(O)=O)CC1)(C3=CC=C(Cl)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.
      Select Batch:
      Purity: 98%
    • 产品描述: MK-0752 是一种高效、口服活性的特异性 γ-分泌酶(γ-secretase)抑制剂,对人 SH-SY5Y 细胞 Aβ40 呈剂量依赖性降低,IC50为 5 nM。MK-0752 穿过血脑屏障。MK-0752 降低体内新生的中枢神经系统 Aβ。
      IC50和靶点:
      In Vitro:
      In Vivo:
      Clinical Trial:
      Solvent & Solubility:
    • Andersson, E.R., and Lendahl, U.Therapeutic modulation of Notch signalling - are we there yet?Nat. Rev. Drug Discov.13(5),357-378(2014)

      Jurisch-Yaksi, N., Sannerud, R., and Annaert, W.A fast growing spectrum of biological functions of γ-secretase in development and diseaseBiochim. Biophys. Acta1828(12),2815-2827(2013)

      Matthews, C.Z., and Woolf, E.J.Determination of a novel gamma-secretase inhibitor in human plasma and cerebrospinal fluid using automated 96 well solid phase extraction and liquid chromatography/tandem mass spectrometryJ. Chromatogr. B Analyt. Technol. Biomed. Life Sci.863(1),36-45(2008)

      Cook, J.J., Wildsmith, K.R., Gilberto, D.B., et al.Acute γ-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-β production to alternative APP fragments without amyloid-β reboundJ. Neurosci.30(19),6743-6750(2010)

      Schott, A.F., Landis, M.D., Dontu, G., et al.Preclinical and clinical studies of gamma secretase inhibitors with docetaxel on human breast tumorsClin. Cancer Res.19(6),1512-1524(2013)

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