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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Stearoyl-CoA Desaturase (SCD)-MK-8245 trifluoroacetate
MK-8245 trifluoroacetate

Chemical Structure : MK-8245 trifluoroacetate

CAS No.: 1415559-41-9

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MK-8245 trifluoroacetate (MK 8245 Trifluoroacetate; MK8245 Trifluoroacetate)

货号: PC-43378Not For Human Use, Lab Use Only.

MK-8245 trifluoroacetate is a potent, selective liver-targeted stearoyl-CoA desaturase (SCD) inhibitor with IC50 of 3, 3 and 1 nM for rat, mouse and human SCD1 enzyme, respectively.

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5 mg ￥1180 In stock
10 mg ￥1780 In stock
25 mg ￥2980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MK-8245 trifluoroacetate is a potent, selective liver-targeted stearoyl-CoA desaturase (SCD) inhibitor with IC50 of 3, 3 and 1 nM for rat, mouse and human SCD1 enzyme, respectively.
MK-8245 displays highly selective over the Δ-5 and Δ-6 desaturases (IC50>100 uM).
MK-8245 has IC50 values of 68 nM and 1066 nM in Hum HepG2 and rat hepatocyte assays, demonstrates HepG2/hepatocyte ratio of 16:1.
MK-8245 exhibits preclinical antidiabetic and antidyslipidemic efficacy in vivo, demonstrats maximal liver SCD inhibition while sparing inhibition in the skin and eye tissues associated with adverse events.

物理化学性质&存储条件

分子量 581.2725
分子式 C19H17BrF4N6O6
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2H-Tetrazole-2-acetic acid, 5-[3-[4-(2-bromo-5-fluorophenoxy)-1-piperidinyl]-5-isoxazolyl]-, 2,2,2-trifluoroacetate (1:1)

参考文献

1. Oballa RM, et al. J Med Chem. 2011 Jul 28;54(14):5082-96.

2. Landry F, et al. J Lipid Res. 2011 Aug;52(8):1494-9.

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