化合物MK-8245 T2650

Product Introduction
Bioactivity


英文名: MK-8245

描述: MK8245 是肝靶向的硬脂酰 -CoA 去饱和酶(SCD)抑制剂，对人 SCD1 和鼠 SCD1 的IC50值分别为 1 nM 和 3 nM，具有抗糖尿病和抗血脂异常的作用。

激酶实验: High Throughput Screening: FITC-MBM1 at 15 nM and menin at 150 nM in the FP buffer are mixed and incubated for 1h in the dark at room temperature. For point screening, the 0.2 μL of each compound (20 μM final concentration, 1% DMSO) is added to 20 μL of the aliquot of the protein-peptide mixture and incubated on 384-well plates in the dark at room temperature for 1h. In confirmation screening, the serial dilution plates with compounds in DMSO are prepared and used to titrate the menin-FITC-MBM1 complex. Change in fluorescence polarization is monitored at 525 nm after excitations at 495 nm using the PHERAstar microplate reader (BMG) and applied to determine IC50 values with the Origin 7.0 program.

体外活性: 在小鼠,大鼠,,犬和猕猴中,MK-8245（p.o.）的主要作用部位是肝脏,但对潜在的不良反应相关组织几乎无效.在eDIO鼠中,MK-8245剂量依赖性影响糖筛选,提高糖清除力（ED50：7 mg/kg）.

体内活性: 在大鼠含有功能性活性OATPs的肝细胞实验,MK-8245对SCD有较强抑制效果（IC50：68 nM）,但在缺乏活性OATPs的HepG2细胞实验中效果较弱（IC50：1 μM）。在HepG 实验中,MK-8245对Δ-5和Δ-6脱饱和酶的选择性很高。MK-824含有四氮唑乙酸基团,具有OATPs识别和肝靶向功能。

存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 86 mg/mL (184.1 mM)


关键字: Inhibitor | Stearoyl-CoA Desaturase (SCD) | MK-8245 | MK8245 | MK 8245 | inhibit

相关产品: 6''-O-Acetylglycitin | JX06 | DS-1001b | (R)-GNE-140 | CBR-5884 | LW6 | ALDH1A3-IN-3 | DHODH-IN-13 | IDH2R140Q-IN-2 | WAY-311610

相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Clinical Compound Library | Fluorochemical Library | Inhibitor Library | Anti-Obesity Compound Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途