2. GPCR/G Protein
  3. GLP Receptor
  4. GLP-1R agonist 30

GLP-1R agonist 30 是一种具有口服活性和选择性的 GLP-1R 激动剂，其 EC50 为 0.048 nM。GLP-1R agonist 30 具有优异的选择性，对 GLP-2R、GIPR 和 GCPR 的 EC50 均大于 20 μM。GLP-1R agonist 30 显著增强 cAMP 刺激活性并降低 hERG 抑制活性。GLP-1R agonist 30 具有良好的吸收率和优异的 β-arrestin 通路选择性。GLP-1R agonist 30 可有效改善 B-hGLP1R 基因敲入小鼠的葡萄糖耐受性并促进胰岛素分泌。

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GLP-1R agonist 30 Chemical Structure

GLP-1R agonist 30 Chemical Structure

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GLP-1R agonist 30 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

GLP-1R agonist 30 is a selective and orally active GLP-1R agonist with an EC50 of 0.048 nM. GLP-1R has excellent selectivity, with EC50 greater than 20 μM for GLP-2R, GIPR, and GCPR. GLP-1R agonist significantly increases cAMP-stimulating activity while markedly reducing hERG inhibitory activities. GLP-1R agonist has preferable absorption and excellent β-arrestin pathway selectivity. GLP-1R agonist effectively improves glucose tolerance and promoted insulin secretion in B-hGLP1R knock-in mice[1].

IC50 & Target

0.048 nM
体外研究
(In Vitro)

GLP-1R agonist (Compound 73) 显著抑制 CHO 细胞中 hERG 活性，药物浓度为 10 μM 时 hERG 抑制率为 37.6%，1 μM 时为 0.6%[1]。
GLP-1R agonist 具有优异的通路选择性和弱的 β-arrestin 激动剂活性，在 HEK293 细胞中对 β-arrestin1 和 β-arrestin2 的 EC50 分别为 863.70 nM和 2021.00 nM[1]。
GLP-1R agonist 对 GLP-1R 具有优异的结合能力，在 CHO 细胞中，药物浓度为 500 nM 时结合率为 35.46%，5000 nM 时结合率为 71.21%[1]。
GLP-1R agonist 具有出色的选择性，在 CHO 细胞中对 GLP-2R、GIPR 和 GCPR 的 EC50 均大于 20 μM，且在 Endoc-βh5 细胞中具有可靠的胰岛素释放促进能力 (EC50：22.705 nM)[1]。

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

GLP-1R agonist 30 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose SampleTime Route Indicator value
Rat 5 mg/kg 0.25, 0.5, 1, 2, 4, 8 and 24 h p.o. T1/2 3.32 hr
Rat 5 mg/kg 0.25, 0.5, 1, 2, 4, 8 and 24 h p.o. Tmax 2.67 hr
Rat 5 mg/kg 0.25, 0.5, 1, 2, 4, 8 and 24 h p.o. Cmax 256.40 ng/mL
Rat 5 mg/kg 0.25, 0.5, 1, 2, 4, 8 and 24 h p.o. AUC0-inf 1377.38 ng·h/mL
Rat 5 mg/kg 0.25, 0.5, 1, 2, 4, 8 and 24 h p.o. F 54.25 %
Rat 5 mg/kg 0.25, 0.5, 1, 2, 4, 8 and 24 h p.o. CL/F 65.85 mL/min/kg
体内研究
(In Vivo)

GLP-1R agonist (Compound 73) (1-10 mg/kg，口服，15 分钟后给予葡萄糖) 剂量依赖性地降低 hGLP-1R 敲入小鼠的血糖水平并增加葡萄糖刺激的胰岛素分泌[1]。

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

Animal Model: male B-hGLP1R knock-in mice (12 weeks old) were injected intraperitoneally with 2 g/kg 40% (w/v) dextrose(D-Glucose) ( HY-B0389) 15 min after drugs administration[1].
Dosage: 1, 10 mg/kg
Administration: oral gavage (p.o.), followed by dextrose administration 15 minutes later, and then collects blood from a tail nick at designated time points (15 min before and 0, 15, 30, 60, and 120 min after dextrose administration)
Result: Dose-dependently decreased blood glucose level and increased glucose-stimulated insulin secretion in hGLP-1R knock-in mice.
分子量

619.63

Formula

C33H32F3N5O4
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

GLP-1R agonist 30 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GLP-1R agonist 30GLP ReceptorGlucagon-Like Peptide-1 Receptor (GLP-1R)Human ether-a-go-go-related gene (hERG)AgonistsCHO cellsEndoc-βh5 cellsB-hGLP1R knock-in miceInhibitorinhibitorinhibit

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