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MLN-4760
CAS No. 305335-31-3
MLN-4760( MLN4760 | MLN 4760 )
Catalog No. M13970 CAS No. 305335-31-3
MLN-4760 (MLN4760) is a potent, selective inhibitor of angiotensin-converting enzyme (ACE)-related carboxypeptidase ACE2 with IC50 of 0.44 nM (hACE2).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 357 | Get Quote |
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| 10MG | 537 | Get Quote |
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| 25MG | 858 | Get Quote |
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| 50MG | 1161 | Get Quote |
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| 100MG | 1557 | Get Quote |
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| 200MG | Get Quote | Get Quote |
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| 500MG | Get Quote | Get Quote |
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| 1G | Get Quote | Get Quote |
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Biological Information
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Product NameMLN-4760
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NoteResearch use only, not for human use.
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Brief DescriptionMLN-4760 (MLN4760) is a potent, selective inhibitor of angiotensin-converting enzyme (ACE)-related carboxypeptidase ACE2 with IC50 of 0.44 nM (hACE2).
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DescriptionMLN-4760 (MLN4760) is a potent, selective inhibitor of angiotensin-converting enzyme (ACE)-related carboxypeptidase ACE2 with IC50 of 0.44 nM (hACE2); displays >5,000-fold selectivity over related enzymes including human testicular ACE (IC50>100 uM) and bovine carboxypeptidase A (IC50=27 uM); exacerbated the Ang II-dependent formation of ROS and abolished the generation of Ang-(1-7) from Ang II; exacerbates cardiac hypertrophy and fibrosis in Ren-2 hypertensive rats.Obesity Phase 1 Discontinued(In Vitro):MLN-4760 is a potent and selective human ACE2 inhibitor (IC50, 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes human testicular ACE (IC50, >100 μM) and bovine carboxypeptidase A (CPDA; IC50, 27 μM). MLN-4760 effectively quenches cleavage of the 7-Mca-YVADAPK(Dnp) in rhACE2. MLN-4760 shows pIC50 at rhACE2 of 8.5±0.1 and at rhACE of 4.4±0.2. MLN-4760 also shows pIC50 at rhACE2 of 4.7±0.1, 6.9±0.1 and at ACE of 4.4±0.1, 6.2±0.1 in murine heart and mononuclear cells (MNCs), resepctively.(In Vivo):MLN-4760 (100 μM, intracerebroventricular infusion for five days) significantly worsens neurological function at 4 h and 3 d post-stroke without significantly increasing infarct volume.
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In VitroMLN-4760 is a potent and selective human ACE2 inhibitor (IC50, 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes human testicular ACE (IC50, >100 μM) and bovine carboxypeptidase A (CPDA; IC50, 27 μM). MLN-4760 effectively quenches cleavage of the 7-Mca-YVADAPK(Dnp) in rhACE2. MLN-4760 shows pIC50 at rhACE2 of 8.5±0.1 and at rhACE of 4.4±0.2. MLN-4760 also shows pIC50 at rhACE2 of 4.7±0.1, 6.9±0.1 and at ACE of 4.4±0.1, 6.2±0.1 in murine heart and mononuclear cells (MNCs), resepctively.
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In VivoMLN-4760 (100 μM, intracerebroventricular infusion for five days) significantly worsens neurological function at 4 h and 3 d post-stroke without significantly increasing infarct volume.
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SynonymsMLN4760 | MLN 4760
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PathwayMetabolic Enzyme/Protease
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TargetACE
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RecptorACE
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Research AreaMetabolic Disease
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IndicationObesity
Chemical Information
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CAS Number305335-31-3
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Formula Weight428.31
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Molecular FormulaC19H23Cl2N3O4
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Purity>98% (HPLC)
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SolubilityIn Vitro:?H2O : 100 mg/mL (233.48 mM)
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SMILESCC(C)C[C@H](N[C@@H](CC1=CN=CN1CC2=CC(Cl)=CC(Cl)=C2)C(O)=O)C(O)=O
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Chemical Name(S,S)-2-[1-carboxy-2-[3-(3,5-dichlorobenzyl)-3H-imidazol4-yl]-ethylamino]-4-methylpentanoic acid
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Towler P, et al. J Biol Chem. 2004 Apr 23;279(17):17996-8007.
2. Dales NA, et al. J Am Chem Soc. 2002 Oct 9;124(40):11852-3.
3. Ye M, et al. Hypertension. 2012 Sep;60(3):730-40.
4. Joshi S, et al. Eur J Pharmacol. 2016 Mar 5;774:25-33.
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