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530616 ACE2 Inhibitor, MLN-4760 - CAS 305335-31-3 - Calbiochem

Overview

Key Specifications Table

CAS #Empirical Formula
305335-31-3C₁₉H₂₃Cl₂N₃O₄

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5.30616.0001
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      Glass bottle 2 mg
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      Description
      OverviewA cell-permeable, bioavailable, highly potent, inhibitor of angiotensin converting enzyme 2 (ACE2; IC50 = 440 pM against soluble human ACE2) that exhibits far greater selectivity over bovine bovine carboxypeptidase A and porcine ACE (IC50 = 27 and >100 µM, respectively). Binds to the active site zinc with high-affinity and emulates the transition state during peptide hydrolysis. Reduces serum and kidney ACE 2 activity and abolishes angiotensin II-induced hypertension in mice. Shown to selectively block ANG-(1-7) formation in ACE2 WT mice subjected to low ANG II concentrations (<0.1 µM), but at higher ANG II concentrations it does not affect ANG -(1-7) levels in mice.
      Catalogue Number530616
      Brand Family Calbiochem®
      Synonyms(S,S)-2-(1-Carboxy-2-(3-(3,5-dichlorobenzyl)-3H-imidazol-4-yl)-ethylamino)-4-methylpentanoic acid, 2(S)-(1(S)-Carboxy-2-(3-(3,5-dichlorobenzyl)-3H-imidazol-4-yl)-ethylamino)-4-methylpentanoic acid, Angiotensin-Converting Enzyme-Related Carboxypeptidase Inhibitor, ML00106791, GL-1001, GL1001, MLN4760
      References
      ReferencesTikellis, C., et al. 2014. Am. J. Physiol. Renal Physiol. 306, F773.
      Grobe, N., et al. 2013. Am. J. Physiol. Cell Physiol 304, C945.
      Ye, M., et al. 2012. Hypertension 60, 730.
      Dilauro, M., et al. 2010. Am. J. Physiol. Renal Physiol. 298, F1523.
      Thomas, M.C., et al. 2010. Circ. Res. 107, 888.
      Trask, A.J., et al. 2010. Am. J. Hypertens. 23, 687.
      Byrnes, J.J., et al. 2009. Inflamm. Res. 58, 819.
      Soler, M.J., et al. 2007. Kidney Int. 72, 614.
      Towler, P., et al. 2004. J. Biol. Chem. 279, 17996.
      Dales, N.A., et al. 2002. J. Am. Chem. Soc. 124, 11852.
      Product Information
      CAS number305335-31-3
      FormWhite powder
      Hill FormulaC₁₉H₂₃Cl₂N₃O₄
      Chemical formulaC₁₉H₂₃Cl₂N₃O₄
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary Targetsoluble human ACE2
      Primary Target IC<sub>50</sub>440 pM for soluble human ACE2
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalog Number GTIN
      5.30616.0001 04055977260960