D5D-IN-326是一种选择性、可口服的delta-5desaturase(D5D)抑制剂，在酶实验和细胞实验中，分别对大鼠和人D5D的IC50值为72和22nM，对D6D或D9D的活性无影响。在食物诱导的C57BL/6J肥胖小鼠中，D5D-IN-326能够降低胰岛素耐受性，并且减轻小鼠体重。
D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC50s 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 reduces insulin resistance and decreases body weight in diet-induced obese C57BL/6J mice[1].
D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC50s 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[1].
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[1].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[1].
[1]. Yashiro H, et al. A Novel Selective Inhibitor of Delta-5 Desaturase Lowers Insulin Resistance and Reduces Body Weight in Diet-Induced Obese C57BL/6J Mice. PLoS One. 2016 Nov 10;11(11):e0166198.
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