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Hydroxy bosentan

Cat. No.:YN370922

  • CAS No. :253688-60-7

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    • 生物活性
    • 参考文献
    • 产品名称: Hydroxy bosentan
      CAS No.: 253688-60-7
      Chemical Name: 4-(2-hydroxy-1,1-dimethylethyl)-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2'-bipyrimidin]-4-yl]-benzenesulfonamide
      Synonyms:Ro 48-5033
      分子量:567.61
      分子式:C₂₇H₂₉N₅O₇S
      SMILES:COC1=CC=CC=C1OC2=C(N=C(N=C2OCCO)C3=NC=CC=N3)NS(C4=CC=C(C=C4)C(CO)(C)C)(=O)=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: Hydroxy bosentan (Ro 48-5033) 是 Bosentan (BOS) 被肝脏中的细胞色素 P450 系统代谢的后的主要代谢产物。Ro 48-5033 在药理上协助 BOS,保留 10%-20% 的活性。
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    • Lepri, S., Goracci, L., Valeri, A., et al.Metabolism study and biological evaluation of bosentan derivativesEur. J. Med. Chem.121,658-670(2016)

      Fahrmayr, C., König, J., Auge, D., et al.Phase I and II metabolism and MRP2-mediated export of bosentan in a MDCKII-OATP1B1-CYP3A4-UGT1A1-MRP2 quadruple-transfected cell lineBr. J. Pharmacol.169(1),21-33(2013)

      Jae, H.S., Winn, M., Dixon, D.B., et al.Pyrrolidine-3-carboxylic acids as endothelin antagonists. 2. Sulfonamide-based ETA/ETB mixed antagonistsJ. Med. Chem.40(20),3217-3227(1997)

      Wu, C., Decker, E.R., Blok, H., et al.Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)-thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonistJ. Med. Chem.47(8),1969-1986(2004)

      Dingemanse, J., and van Giergsbergen, L.M.Clinical pharmacology of bosentan, a dual endothelin receptor antagonistClin. Pharmacokinet.43(15),1089-1115(2004)

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