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504044 PrCP Inhibitor - CAS 1252037-41-4 - Calbiochem

Overview

Key Spec Table

CAS #Empirical Formula
1252037-41-4C₃₁H₃₃Cl₂N₅O₂

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      Glass bottle 10 mg
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      Description
      OverviewA dichlorobenzimidazolopyrrolidinamide compound that acts as a highly potent PrCP-selective inhibitor (IC50 = 1 nM against human PrCP; IC50 = 2 and 8 nM against mouse PrCP, respectively, in the absence or presence of 1% mouse serum albumin), presumably via non-covalent catalytic site interaction, while exhibiting no significant potency toward panels of ion channels, receptors, and enzymes, including homologous serine proteases QPP, FAP, PEP, ACE2, DPP4, DPP8, and DPP9 (IC50 >25 µM). Oral administration (100 mg/kg/d for 5 d) is reported to result in significant food intake reduction and body fat loss among high fat diet-induced obese mice in vivo.
      Catalogue Number504044
      Brand Family Calbiochem®
      SynonymsAngiotensinase C Inhibitor, Lysosomal Carboxypeptidase C Inhibitor, Lysosomal Pro-X Carboxypeptidase Inhibitor, PCP Inhibitor, Proline Carboxypeptidase Inhibitor, Prolylcarboxypeptidase Inhibitor, 2-Amino-N-((2S,3S)-3-(biphenyl-4-yl)-1-((2S)-2-(5,6-dichloro-1H-benzimidazol-2-yl)pyrrolidin-1-yl)-1-oxobutan-2-yl)-2-methylpropanamide
      References
      ReferencesWu, Z., et al. 2012. Bioorg. Med. Chem. Lett. 22, 1774.
      Graham, T.H., et al. 2012. Bioorg. Med. Chem. Lett. 22, 658.
      Zhou, C., et al. 2010. J. Med. Chem. 53, 7251.
      Product Information
      CAS number1252037-41-4
      FormWhite powder
      Hill FormulaC₃₁H₃₃Cl₂N₅O₂
      Chemical formulaC₃₁H₃₃Cl₂N₅O₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Primary TargetPrCP
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage -20°C
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      5040440001 04055977264265