1236767-85-3
1236767-85-3 結(jié)構(gòu)式
基本信息
D-5D-IN-326,D5D IN 326,D5DIN326
3H-Pyrrolo[2,3-d]pyrimidine-4,6-dione, 5,7-dihydro-2-(2,2,3,3,3-pentafluoropropoxy)-3-[4-(2,2,2-trifluoroethoxy)phenyl]-
常見問題列表
IC50: 72 nM (Rat D5D), 22 nM (Human D5D)
D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC 50 s of 72 and 22 nM for rat and human D5D in enzymic and cell-based assays, respectively, has no effect on D6D or D9D activity.
D5D-IN-326 (0.1, 1, and 10 mg/kg, p.o. for 6 weeks) gradually decreases body weight at 10 mg/kg, but lowers doses are not effective in DIO mice after treatment for 6 weeks.
D5D-IN-326 (10 mg/kg, p.o. for 6 weeks) also significantly decreases gene expression levels of
Ccl2
,
Cd68
,
Adgre1
, and
Il6
, decreases epididymal
Lep
and
Adipoq
mRNAs which are significantly increased in HFD DIO mice.