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

530616
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Tabulka spec. kláve

CAS #Empirical Formula
305335-31-3C₁₉H₂₃Cl₂N₃O₄

Products

Katalogové čísloBalení ks/bal.
5.30616.0001 Skleněná láhev 2 mg
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
Katalogové číslo GTIN
5.30616.0001 04055977260960