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

530616
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Empirical FormulaCAS #
C₁₉H₂₃Cl₂N₃O₄ 305335-31-3

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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®
      SynonymsGL-1001, GL1001, MLN4760, (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
      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
      Applications
      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
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications

      Documentation

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

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Tikellis, 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.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision04-June-2014 JSW
      SynonymsGL-1001, GL1001, MLN4760, (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
      DescriptionA selective and highly potent inhibitor against ACE2 carboxypeptidase activity (IC50 = 0.44 nM against 50 pM human ACE2; [ZnCl2] = 10 µM, [MCA-APK(DNP)] = 50 µM) with little potency toward carboxypeptidase A or ACE peptidyldipeptidase activity (IC50 = 27 µM and >100 µM against 0.5 nM bovine CPDA and 1 nM porcine ACE, respectively; [Substrate] = 50 µM). Enhances TNF- (10 pg/mL) stimulated expression of proinflammatory cytokines in murine endothelial cells (1 µM using SVEC-40 line and primary aorta endothelial cultures) in vitro and is widely employed for studying ACE2 involvement in kidney, cardiovascular, and inflammatory bowel diseases via drinking water (10 mg/kg/d), i.v. (0.1 mg/kg), and s.c. (30 mg/kg/d to 300 mg/kg/12 h) injection in rats and mice in vivo. The inhibitor Leucine moiety is shown to simultaneously target ACE2 substrate S1 pocket with its isobutyl group and active site zinc via its carboxylate, while the compound′s 3,5-dichlorobenzyl group effectively occupy S1′ subsite.
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number305335-31-3
      Chemical formulaC₁₉H₂₃Cl₂N₃O₄
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage +2°C to +8°C
      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.
      Toxicity Standard Handling
      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.