ELOVL6-IN-1 是一种选择性ELOVL6抑制剂,口服具有活性。它对丙二酰辅酶 a (Ki:994 nM) 和对棕榈酰辅酶 a 具有非竞争性抑制 ELOVL6 作用。它能够剂量依赖性的一种小鼠ELOVL6(IC50:0.350 μM)。
产品描述
ELOVL6-IN-1 is a potent, orally active and selective ELOVL6 inhibitor. ELOVL6-IN-1 dose-dependently inhibits mouse ELOVL6 activities, with an IC50 value of 0.350 μM. ELOVL6-IN-1 inhibits ELOVL6 in a noncompetitive manner for malonyl-CoA (Ki=994 nM) and palmitoyl-CoA[1].
体外活性
ELOVL6-IN-1 has sufficiently lipophilic. It has the potential to penetrate the intracellular space in a passive diffusion manner potentially[1].
体内活性
ELOVL6-IN-1 (10 mg/kg; p.o.; 0~2 hours) displays appreciable plasma and liver exposure[1].
ELOVL6-IN-1 (10 and 30 mg/kg; p.o.; 0~2 hours) reduces the elongation index of the liver lipids[1].
ELOVL6-IN-1 (100 mg/kg; p.o.; 2 days) reduces the elongation index of the total fatty acids of the liver[1].
Cas No.
1185736-98-4
分子式
C27H24F3N3O3
分子量
495.502
别名
ELOVL6-IN-1
储存和溶解度
DMSO:45 mg/mL (90.82 mM,Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years