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

530616
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₉H₂₃Cl₂N₃O₄ 305335-31-3

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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
          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
          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
          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.