MK-8245 trifluoroacetate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MK-8245 三氟乙酸酯是一种有效的、选择性的肝靶向硬脂酰辅酶A去饱和酶 (SCD) 抑制剂，对大鼠、小鼠和人 SCD1 酶的 IC50 分别为 3、3 和 1 nM。

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; displays highly selective over the Δ-5 and Δ-6 desaturases (IC50>100 uM); has IC50 values of 68 nM and 1066 nM in Hum HepG2 and rat hepatocyte assays, demonstrates HepG2/hepatocyte ratio of 16:1; 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.Diabetes Phase 1 Discontinued.

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MK 8245 Trifluoroacetate | MK8245 Trifluoroacetate

Metabolic Enzyme/Protease

SCD

SCD

Metabolic Disease

Diabetes

1415559-41-9

581.2725

C19H17BrF4N6O6

>98% (HPLC)

10 mM in DMSO

C1CN(CCC1OC2=C(C=CC(=C2)F)Br)C3=NOC(=C3)C4=NN(N=N4)CC(=O)O.C(=O)(C(F)(F)F)O

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

(-20℃)

With Ice Pack

≥ 2 years