ELOVL6-IN-3

CAS: 712346-06-0 F: C27H24F3N3O3 W: 495.49

ELOVL6-IN-1 is a potent, orally active and selective ELOVL6 inhibitor. ELOVL6-IN-1 dose-dependently inhibits mouse ELOVL

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Bioactivity	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].
Target	IC50: 0.35 μM (ELOVL6), Ki: 994 nM (ELOVL6)
Invitro	ELOVL6-IN-1 具有足够的亲脂性，具有以被动扩散方式穿透细胞内空间的潜力[1]。
In Vivo	ELOVL6-IN-1 (10 mg/kg；口服；0~2 小时) 显示出明显的血浆和肝脏暴露[1]。 ELOVL6-IN-1 (10 和 30 mg/kg；口服；0~2 hours) 降低肝脂质的延伸指数[1]。 ELOVL6-IN-1 (100 mg/kg；口服；2 天) 降低肝脏总脂肪酸的延伸指数[1]。
Name	ELOVL6-IN-3
CAS	712346-06-0
Formula	C27H24F3N3O3
Molar Mass	495.49
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Shimamura K, et al. 5,5-Dimethyl-3-(5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-1-phenyl-3-(trifluoromethyl)-3,5,6,7-tetrahydro-1H-indole-2,4-dione, a potent inhibitor for mammalian elongase of long-chain fatty acids family 6: examination of its potential utility as a pharmacological tool. J Pharmacol Exp Ther. 2009;330(1):249-256. [2]. Takahashi T, Nagase T, Sasaki T, et al. Synthesis and evaluation of a novel indoledione class of long chain fatty acid elongase 6 (ELOVL6) inhibitors. J Med Chem. 2009;52(10):3142-3145. [3]. Zheng Junxia, Wu Zhiwei, Dai Mibei, Xu Zhihui, Li Xiaomei, Zhu Shanshan, Lin Chuyun, Hu Peijian, Zhang Luo, Huang Huarong, Zhao Suqing, Zhang Kun and Sun Pinghua, Quantitative Structure Activity Relationship Studies on a Novel Indolediones as Long Chain Fatty Acid Elongase 6 (ELOVL6) Inhibitors, Letters in Drug Design & Discovery 2011; 8(5) .

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