2. GPCR/G Protein
  3. G protein-coupled Bile Acid Receptor 1
  4. TGR5 agonist 10

TGR5 agonist 10 TGR5 agonist 10 是一种选择性、变构且口服有效的武田 G 蛋白偶联受体 5 (TGR5) 激动剂，对人 TGR5 和小鼠 TGR5 的 EC50 值分别为 0.8 μM 和 0.6 μM。TGR5 agonist 10 TGR5 agonist 10 表现出相对于 FXR 的 TGR5 选择性。TGR5 agonist 10 可激活 hTGR5 和 mTGR5 以诱导 cAMP 积累，并能正向调节石胆酸在 hTGR5 上的功能活性和效力，且在 cAMP 形成方面的选择性高于 β-抑制蛋白 2 招募。TGR5 agonist 10 在 Mus musculus 口服葡萄糖耐量试验中发挥降糖作用。TGR5 agonist 10 可用于糖尿病的研究。

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TGR5 agonist 10

TGR5 agonist 10 Chemical Structure

CAS No. : 3081614-92-5

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TGR5 agonist 10 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TGR5 agonist 10 is a selective, allosteric and orally active Takeda G protein coupled receptor 5 (TGR5) agonist with EC50s of 0.8 μM and 0.6 μM for human TGR5 and mouse TGR5, respectively. TGR5 agonist 10 demonstrates selectivity for TGR5 over FXR. TGR5 agonist 10 activates hTGR5 and mTGR5 to induce cAMP accumulation, and positively modulates lithocholic acid functional activity and potency at hTGR5, with higher selectivity for cAMP formation over β-arrestin2 recruitment. TGR5 agonist 10 exerts glucose-lowering effects in Mus musculus oral glucose tolerance tests. TGR5 agonist 10 can be used for the research of diabetes[1].

IC50 & Target[1]

Human TGR5

0.8 μM (EC50)

Mouse TGR5

0.6 μM (EC50)

体外研究
(In Vitro)

TGR5 agonist 10 (compound A1) 对 β-arrestin2 募集的活性较低 (EC50 = 26.5 μM)，弱于其在 HEK293T 细胞中对 cAMP 积累的活性[1]。
TGR5 agonist 10 (10-20 μM；作用 8 小时) 在 HEK293T 细胞中，于 10 μM 或 20 μM 浓度下均不会激活 FXR，表明其对 TGR5 具有选择性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

TGR5 agonist 10 相关抗体:
体内研究
(In Vivo)

TGR5 agonist 10 (compound A1) (100 mg/kg；灌胃给药) 在 ICR 小鼠的 OGTT 模型中表现出显著的降血糖作用[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ICR (8-week-old, wild-type) receiving 3 g/kg oral glucose[1]
Dosage: 100 mg/kg
Administration: p.o.; single dose (30 minutes before glucose challenge)
Result: Showed significant glucose-lowering effects in the oral glucose tolerance test (OGTT), with comparable efficacy to positive control metformin.
分子量

436.58

Formula

C25H40O6
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

TGR5 agonist 10 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

TGR5 agonist 103081614-92-5G protein-coupled Bile Acid Receptor 1G-protein coupled receptor 19GPCR19TGR5GPBAR1HEK293T cellsICR miceβ-arrestin2farnesoid X receptordiabetesmTGR5cAMPlithocholic acidFXRhTGR5Inhibitorinhibitorinhibit

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