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Merck
모든 사진(1)

주요 문서

5.30616

Sigma-Aldrich

ACE2 Inhibitor, MLN-4760

≥97% (HPLC), powder, Calbiochem®

동의어(들):

ACE2 Inhibitor, MLN-4760, ( 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

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About This Item

실험식(Hill 표기법):
C19H23Cl2N3O4
CAS Number:
Molecular Weight:
428.31
MDL number:
UNSPSC 코드:
51111800
NACRES:
NA.77

Quality Level

분석

≥97% (HPLC)

양식

powder

제조업체/상표

Calbiochem®

저장 조건

OK to freeze
protect from light

기술

inhibition assay: suitable

색상

white

solubility

DMSO: 100 mg/mL

저장 온도

2-8°C

SMILES string

Clc1cc(cc(c1)C[n]2cncc2C[C@H](N[C@@H](CC(C)C)C(=O)O)C(=O)O)Cl

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

InChI key

NTCCRGGIJNDEAB-IRXDYDNUSA-N

일반 설명

MLN-4760 is a highly potent and selective cell-permeable inhibitor of angiotensin converting enzyme 2, which is its primary target. (ACE2; IC50 = 440 pM against soluble human ACE2).

생화학적/생리학적 작용

MLN-4760 is bioavailable and exhibits far greater selectivity for carboxypeptidase (IC50 = 0.44 nM against 50 pM human ACE2; [ZnCl2] = 10 μM, [MCA-APK(DNP)] = 50 μM) over bovine 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) and porcine ACE (IC50 = 27 and >100 μM, respectively). This reversible ACE2 inhibitor binds to the active site zinc with high-affinity and emulates the transition state during peptide hydrolysis. It reduces serum and kidney ACE 2 activity and abolishes angiotensin II-induced hypertension in mice. MLN-4760 selectively blocks angiotensin (ANG-(1-7)) formation in ACE2 wild type (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. This ACE2 inhibitor enhances tumor necrosis factor (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. MLN-4760 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.
MLN-4760 also enables to study the effect of reduced ACE2 activity on the lung′s susceptibility for Coronavirus disease (COVID) related acute respiratory distress syndrome (ARDS).

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

법적 정보

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

John J Byrnes et al.
Inflammation research : official journal of the European Histamine Research Society ... [et al.], 58(11), 819-827 (2009-06-12)
Angiotensin-converting enzyme 2 (ACE2) is expressed in gastrointestinal tissue. Previous studies of GL1001, a potent and selective ACE2 inhibitor, have revealed anti-inflammatory activity in the mouse digestive tract. We hypothesized that GL1001 might also produce beneficial effects in a mouse
Nadja Grobe et al.
American journal of physiology. Cell physiology, 304(10), C945-C953 (2013-02-09)
Angiotensin-converting enzyme 2 (ACE2) catalyzes conversion of ANG II to ANG-(1-7). The present study uses newly established proteomic approaches and genetic mouse models to examine the contribution of alternative renal peptidases to ACE2-independent formation of ANG-(1-7). In situ and in
Merlin C Thomas et al.
Circulation research, 107(7), 888-897 (2010-07-31)
Angiotensin-converting enzyme (ACE)2 opposes the actions of angiotensin (Ang) II by degrading it to Ang 1-7. Given the important role of Ang II/Ang 1-7 in atherogenesis, we investigated the impact of ACE2 deficiency on the development of atherosclerosis. C57Bl6, Ace2
Aaron J Trask et al.
American journal of hypertension, 23(6), 687-693 (2010-03-20)
Emerging evidence suggests that cardiac angiotensin-converting enzyme 2 (ACE2) may contribute to the regulation of heart function and hypertension-induced cardiac remodeling. We tested the hypothesis that inhibition of ACE2 in the hearts of (mRen2)27 hypertensive rats may accelerate progression of
Minghao Ye et al.
Hypertension (Dallas, Tex. : 1979), 60(3), 730-740 (2012-07-11)
A newly produced murine recombinant angiotensin (Ang)-converting enzyme 2 (ACE2) was characterized in vivo and in vitro. The effects of available ACE2 inhibitors (MLN-4760 and 2 conformational variants of DX600, linear and cyclic) were also examined. When murine ACE2 was

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