TUG-905

TUG-905 is a potent GPR40 agonist with an pEC50 value of 7.03. TUG-905 increases hypothalamic cell proliferation and survival. TUG-905 reduces body mass and increases the POMC mRNA expression[1][2].

Signaling Pathways >> GPCR/G Protein >> GPR40

Research Areas >> Metabolic Disease

Research Areas >> Neurological Disease

pEC50: 7.03 (GPR40)[1]

TUG-905 (10 µM；7、13 天) 促进细胞增殖和增加神经母细胞标记物 DCX mRNA 水平[2]。 TUG-905 (10 µM；2、4、24 小时) 增加 Neuro2a (鼠神经母细胞瘤) 细胞中的 GPR40、BDNF 基因表达[2]。 Western Blot Analysis[2] Cell Line: DCX/GFAP positive cells (neurospheres from mouse hypothalamic tissue) Concentration: 10 µM Incubation Time: 7 days Result: Increased mRNA levels of the neuroblast marker, DCX, as well as the number of DCX-immunopositive cells.

TUG-905 (2.0 μL，1.0 mM；i.c.v.；每天两次，持续 6 天) 可降低体重并表现出减少热量摄入的趋势[1]。 Animal Model: 6 weeks, Male Swiss mice[1] Dosage: 2.0 μL, 1.0 mM Administration: I.c.v.; twice a day for 6 days Result: Reduced body mass and exhibited a trend toward reducing caloric intake, and induced an increase of IL10 and IL6 in the hypothalamus, and increased the POMC mRNA expression.

[1]. Dragano NRV, et al. Polyunsaturated fatty acid receptors, GPR40 and GPR120, are expressed in the hypothalamus and control energy homeostasis and inflammation. J Neuroinflammation. 2017 Apr 26;14(1):91.  

[2]. Engel DF, et al. Activation of GPR40 induces hypothalamic neurogenesis through p38- and BDNF-dependent mechanisms. Sci Rep. 2020 Jul 6;10(1):11047.