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MedKoo Cat#: 532253 | Name: MLN-4760
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

MLN-4760 is an angiotensin-converting (ACE2) inhibitor. In huMNCs, MLN-4760-B detected 63% ACE2 with 28-fold selectivity over ACE.

Chemical Structure

MLN-4760
CAS#305335-31-3

Theoretical Analysis

MedKoo Cat#: 532253

Name: MLN-4760

CAS#: 305335-31-3

Chemical Formula: C19H23Cl2N3O4

Exact Mass: 427.1066

Molecular Weight: 428.31

Elemental Analysis: C, 53.28; H, 5.41; Cl, 16.55; N, 9.81; O, 14.94

Price and Availability

Size Price Availability Quantity
10mg USD 350.00 2-3 months
25mg USD 550.00 2-3 months
50mg USD 950.00 2-3 months
100mg USD 1,650.00 2-3 months
200mg USD 2,650.00 2-3 months
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Related CAS #
No Data
Synonym
MLN-4760; MLN 4760; MLN4760.
IUPAC/Chemical Name
(2S)-2-[[(2S)-3-[3-[(3,5-dichlorophenyl)methyl]imidazol-4-yl]-1-hydroxy-1-oxopropan-2-yl]amino]-4-methylpentanoic acid
InChi Key
NTCCRGGIJNDEAB-IRXDYDNUSA-N
InChi Code
InChI=1S/C19H23Cl2N3O4/c1-11(2)3-16(18(25)26)23-17(19(27)28)7-15-8-22-10-24(15)9-12-4-13(20)6-14(21)5-12/h4-6,8,10-11,16-17,23H,3,7,9H2,1-2H3,(H,25,26)(H,27,28)/t16-,17-/m0/s1
SMILES Code
CC(C)C[C@H](N[C@@H](CC1=CN=CN1CC2=CC(Cl)=CC(Cl)=C2)C(O)=O)C(O)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
MLN-4760 is a potent and selective human ACE2 inhibitor (IC50, 0.44 nM).
In vitro activity:
MLN-4760 (10−6M) blocked formation of Ang-(1–7) by both mouse rACE2 (Figure 3A) and human rACE2 (Figure 3B). Reference: Hypertension. 2012 Sep;60(3):730-40. https://pubmed.ncbi.nlm.nih.gov/22777933/
In vivo activity:
This study investigated the selected behavioural and hemodynamic parameters in spontaneously hypertensive rats (SHRs) after a 2-week s.c. infusion of MLN-4760 (dose 1 mg/kg/day). MLN-4760 increased plasma hydrogen sulfide (H2S) level and total nitric oxide (NO) synthase activity and conjugated dienes in the brainstem. MLN-4760 administration increased gene expression of Ace2, Sod1, Sod2, Gpx4 and Hmox1, which positively correlated with expression of Nfe2l2 gene encoding the redox-sensitive transcription factor NRF2. Reference: Antioxidants (Basel). 2022 Dec 1;11(12):2385. https://pubmed.ncbi.nlm.nih.gov/36552591/
Solvent mg/mL mM comments
Solubility
DMSO 46.4 108.37
Ethanol 10.0 23.35
Water 86.0 200.79
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 428.31 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Lin Y, Zeng H, Gao L, Gu T, Wang C, Zhang H. Hydrogen Sulfide Attenuates Atherosclerosis in a Partially Ligated Carotid Artery Mouse model via Regulating Angiotensin Converting Enzyme 2 Expression. Front Physiol. 2017 Oct 10;8:782. doi: 10.3389/fphys.2017.00782. PMID: 29066981; PMCID: PMC5641337. 2. Ye M, Wysocki J, Gonzalez-Pacheco FR, Salem M, Evora K, Garcia-Halpin L, Poglitsch M, Schuster M, Batlle D. Murine recombinant angiotensin-converting enzyme 2: effect on angiotensin II-dependent hypertension and distinctive angiotensin-converting enzyme 2 inhibitor characteristics on rodent and human angiotensin-converting enzyme 2. Hypertension. 2012 Sep;60(3):730-40. doi: 10.1161/HYPERTENSIONAHA.112.198622. Epub 2012 Jul 9. PMID: 22777933; PMCID: PMC3426447. 3. Kluknavsky M, Micurova A, Cebova M, Şaman E, Cacanyiova S, Bernatova I. MLN-4760 Induces Oxidative Stress without Blood Pressure and Behavioural Alterations in SHRs: Roles of Nfe2l2 Gene, Nitric Oxide and Hydrogen Sulfide. Antioxidants (Basel). 2022 Dec 1;11(12):2385. doi: 10.3390/antiox11122385. PMID: 36552591; PMCID: PMC9774314. 4. Berenyiova A, Bernatova I, Zemancikova A, Drobna M, Cebova M, Golas S, Balis P, Liskova S, Valaskova Z, Krskova K, Zorad S, Dayar E, Cacanyiova S. Vascular Effects of Low-Dose ACE2 Inhibitor MLN-4760-Benefit or Detriment in Essential Hypertension? Biomedicines. 2021 Dec 24;10(1):38. doi: 10.3390/biomedicines10010038. PMID: 35052717; PMCID: PMC8773407.
In vitro protocol:
1. Lin Y, Zeng H, Gao L, Gu T, Wang C, Zhang H. Hydrogen Sulfide Attenuates Atherosclerosis in a Partially Ligated Carotid Artery Mouse model via Regulating Angiotensin Converting Enzyme 2 Expression. Front Physiol. 2017 Oct 10;8:782. doi: 10.3389/fphys.2017.00782. PMID: 29066981; PMCID: PMC5641337. 2. Ye M, Wysocki J, Gonzalez-Pacheco FR, Salem M, Evora K, Garcia-Halpin L, Poglitsch M, Schuster M, Batlle D. Murine recombinant angiotensin-converting enzyme 2: effect on angiotensin II-dependent hypertension and distinctive angiotensin-converting enzyme 2 inhibitor characteristics on rodent and human angiotensin-converting enzyme 2. Hypertension. 2012 Sep;60(3):730-40. doi: 10.1161/HYPERTENSIONAHA.112.198622. Epub 2012 Jul 9. PMID: 22777933; PMCID: PMC3426447.
In vivo protocol:
1. Kluknavsky M, Micurova A, Cebova M, Şaman E, Cacanyiova S, Bernatova I. MLN-4760 Induces Oxidative Stress without Blood Pressure and Behavioural Alterations in SHRs: Roles of Nfe2l2 Gene, Nitric Oxide and Hydrogen Sulfide. Antioxidants (Basel). 2022 Dec 1;11(12):2385. doi: 10.3390/antiox11122385. PMID: 36552591; PMCID: PMC9774314. 2. Berenyiova A, Bernatova I, Zemancikova A, Drobna M, Cebova M, Golas S, Balis P, Liskova S, Valaskova Z, Krskova K, Zorad S, Dayar E, Cacanyiova S. Vascular Effects of Low-Dose ACE2 Inhibitor MLN-4760-Benefit or Detriment in Essential Hypertension? Biomedicines. 2021 Dec 24;10(1):38. doi: 10.3390/biomedicines10010038. PMID: 35052717; PMCID: PMC8773407.
1: Joshi S, Balasubramanian N, Vasam G, Jarajapu YP. Angiotensin converting enzyme versus angiotensin converting enzyme-2 selectivity of MLN-4760 and DX600 in human and murine bone marrow-derived cells. Eur J Pharmacol. 2016 Mar 5;774:25-33. doi: 10.1016/j.ejphar.2016.01.007. PubMed PMID: 26851370; PubMed Central PMCID: PMC4804635.

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