TGR5 Receptor Agonist (CCDC) 是一种有效的 Takeda G蛋白偶联受体(TGR5; GPCR19)激动剂，在 U2-OS 细胞和黑色素细胞中显示了良好的效力，pEC50分别为 6.8 和 7.5。TGR5 Receptor Agonist 可诱导小鼠外周和中枢对膀胱膨胀的超敏反应，增加细胞内Ca2+浓度。在饮食诱导的肥胖小鼠中，TGR5 Receptor Agonist 还可以减少食物摄入，改善胰岛素反应性。TGR5 Receptor Agonist 可用于糖尿病、膀胱超敏反应和抗肥胖的研究。
| 生物活性 | TGR5 Receptor Agonist (CCDC), a potentTakeda 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 intracellularCa2+concentration. TGR5 Receptor Agonist can also reduces food intake and improvesinsulinresponsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity[1][2][3][4]. |
| IC50& Target | |
体内研究
(In Vivo) | 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 inTrpv1-/-mice[2].
TGR5 Receptor Agonist (CCDC) (2 or 5 μg; ICV) reduces food intake and body weight in diet-induced obese mice[3].
| Animal Model: | Female C57BL/6J mice [12-18 weeks; TRPV1 knockout (trpv1-/-), TRPA1 knockout (trpa1-/-), or TGR5 knockout (Gpbar1-/-)][2] | | 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 inTrpv1-/-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)[3] | | 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)[3] | | 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. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
| 溶解性数据 | In Vitro: DMSO : ≥ 48 mg/mL(132.88 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.7684 mL | 13.8420 mL | 27.6840 mL | | 5 mM | 0.5537 mL | 2.7684 mL | 5.5368 mL | | 10 mM | 0.2768 mL | 1.3842 mL | 2.7684 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 10 mg/mL (27.68 mM); Clear solution
此方案可获得 ≥ 10 mg/mL (27.68 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 100.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 10 mg/mL (27.68 mM); Clear solution
此方案可获得 ≥ 10 mg/mL (27.68 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 100.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
|
m.cnreagent.com