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MLN-4760

Dangerous Goods

CAS number:305335-31-3    molecular formula:C19H23Cl2N3O4

overview

compound introduction

MLN-4760 是一种有效、选择性的人 ACE2 抑制剂,IC50 值为 0.44 nM,对其选择性是对其他相关蛋白的 5000 多倍,包括人睾丸 ACE (IC50,>100 μM) 和牛 carboxypeptidase A (IC50,27 μM) ACE2 (Cell-free assay); CPDA (Cell-free assay) 0.44 nM; 27 μM In vitro conversion from angiotensin II to angiotensin-(1–7) by mouse ACE2 is blocked by MLN-4760 (10 μM). MLN-4760 inhibits both human and mouse ACE2 activity. In huMNCs, MLN-4760-B (an isomer of MLN-4760) detects 63% ACE2 with 28-fold selectivity over ACE. In huCD34+ cells, MLN-4760-B detects 38% of ACE2 activity with 63-fold selectivity. In mu-heart and muMNCs, MLN-4760-B is 100- and 228-fold selective for ACE2, respectively. In muLin- cells, MLN-4760-B detects 25% ACE2 activity with a pIC50 of 6.3. The racemic mixture and MLN-4760-A shows lower efficacy and poor selectivity for ACE2 in MNCs and mu-heart. In vivo MLN-4760 blocks ACE2 activity, thus significantly reverses the elevation of carotid Ang-(1-7) level and the decline of carotid Ang II level induced by NaHS in mice. The anti-atherosclerotic property of NaHS is also significantly abolished by treatment with MLN-4760. Cell Research(from reference) Cell lines:mononuclear cells (MNCs), huCD34+ cells, mu-lineage-depleted (muLin-) cells Concentrations:0.01 nM to 300 μM Incubation Time:1 h, 4 h

Specs

Chinese aliasACE2抑制剂,MLN-4760
English alias(2S)-2-{[(1S)-1-carboxy-2-{1-[(3,5-dichlorophenyl)methyl]-1H-imidazol-5-yl}ethyl]amino}-4-methylpentanoic acid | AKOS040742161 | MS-27570 | UNII-4LD0ZHV25K | (S)-2-(((S)-1-carboxy-2-(1-(3,5-dichlorobenzyl)-1H-imidazol-5-yl)ethyl)amino)-4-methylpentanoic a
CAS number305335-31-3molecular formulaC19H23Cl2N3O4
molecular weight428.31 g/molExact mass-
PSA104.000 Ųlogp1.4

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physicochemical properties

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Safety information

Signal word:
Warning
Hazard Statement:
H302: 吞食有害 H312: 皮肤接触有害 H332: 吸入有害
Statement of Preventive Measures:
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染:用水充分清洗。 P501: 将内容物/容器处理到。。。 P312: 打电话给毒物中心或医生。。。如果你觉得不舒服 P264: 处理后要彻底洗手。 P271: 仅在室外或通风良好的地方使用。 P362: 脱下污染的衣服并洗净后再使用。 P270:

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