产品
编 号：F066960
分子式：C18H14Cl2N2O2
分子量：361.22
分子式：C18H14Cl2N2O2
分子量：361.22
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 1197300-24-5
产品详情
生物活性：
TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity.
体内研究：
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 min
Result: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 (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity.
体内研究：
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 min
Result: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.
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