TGR5

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TGR5 Receptor Agonist 是一种有效的 TGR5(GPCR19) 激动剂，在 U2-OS 细胞测定 (pEC50 = 6.8) 和黑色素细胞 (pEC50 = 7.5) 中显示出更高的效力。

TGR5 Receptor Agonist, a potent TGR5(GPCR19) agonist, showed improved potency in the U2-OS cell assay (pEC50 = 6.8) and in melanophore cells (pEC50 = 7.5).

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TGR5 Receptor Agonist (CCDC) activates directly a sub-population of bladder-innervating dorsal root ganglia (DRG) neurons and a small percentage of non-neuronal cells in Trpv1-/- mice.?TGR5 Receptor Agonist (CCDC) (2?or 5 μg; ICV) reduces food intake and body weight in diet-induced obese mice. Animal Model:Female C57BL/6J mice [12-18 weeks; TRPV1 knockout (trpv1-/-), TRPA1 knockout (trpa1-/-), or TGR5 knockout (Gpbar1-/-)]Dosage:100 μM, 100 μL Administration:Infused gently, to fill but not fully distend the bladder, and allowed to incubate for 5 minResult:Activated directly a sub-population of bladder-innervating dorsal root ganglia (DRG) neurons in Trpv1-/- mice, also activated a small percentage of non-neuronal cells.Increased intracellular Ca2+ in bladder-innervating DRG neurons.Increased intracellular Ca2+ in a small proportion of non-neuronal cells.Animal Model: Male C57BL/6J mice (obese induced by high-fat diet)Dosage:2?or 5 μg at a volume of 0.2 μL per brain side and a rate of 0.6 μL/min Administration:ICV (acute intra-hypothalamic experiment) Result:Significantly reduced food intake over time, with a robust reduction in 24 h food intake and body weight gain.Animal Model:Male C57BL/6J mice (obese induced by high-fat diet; implanted with micro-osmotic pumps that were filled with CCDC)Dosage:5 μg/day; 91.9 μL, pumping rate of 0.09 μL/h Administration:ICV; for 4 weeks (chronic experiment) Result:Reduced food intake and improved insulin responsiveness.Increased energy expenditure during the dark phase.Increased mRNA expression of β1, 2, and 3 adrenoreceptors (Adrb1, Adrb2, and Adrb3) in the epidydimal white adipose tissue, and increased Dio2 (the gene expressing the enzyme D2) in brown adipose tissue.

TGR5 Receptor Agonist | MDK00245 | MDK-00245 | MDK 00245

GPCR/G Protein

GPCR19

TGR5

Metabolic Disease

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1197300-24-5

361.22

C18H14Cl2N2O2

>98% (HPLC)

DMSO, Ethanol: 100 mM

O=C(C1=C(C)ON=C1C2=CC=CC=C2Cl)N(C3=CC=C(Cl)C=C3)C

3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-dimethyl-4-isoxazolecarboxamide

(-20℃)

With Ice Pack

≥ 2 years