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

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.

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GLP-1R agonist 30 Chemical Structure

GLP-1R agonist 30 Chemical Structure

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GLP-1R agonist 30 Related Antibodies

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Description

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
In Vitro

GLP-1R agonist (Compound 73) significantly inhibits hERG activity with hERG inhibition of 37.6% at 10 μM and 0.6% at 1 μM in CHO cells [1].
GLP-1R agonist has superior pathway selectivity and weak β-arrestin agonist activity with EC50 s of 863.70 nM and 2021.00 nM for β-arrestin1 and β-arrestin2 in HEK293 cells[1].
GLP-1R agonist has superior binding capacity on GLP-1R with 35.46% at 500 nM and 71.21% at 5000 nM in CHO cells[1].
GLP-1R has excellent selectivity, with EC50s greater than 20 μM for GLP-2R, GIPR, and GCPR in CHO cells and reliable insulin release promoting ability (EC50: 22.705 nM) in Endoc-βh5 cells[1].

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

GLP-1R agonist 30 Related Antibodies
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
In Vivo

GLP-1R agonist (Compound 73) (1-10 mg/kg, p.o., followed by dextrose administration 15 minutes later) dose-dependently decreases blood glucose level and increases glucose-stimulated insulin secretion in hGLP-1R knock-in mice[1].

MedChemExpress (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.
Molecular Weight

619.63

Formula

C33H32F3N5O4
SMILES

FC1=C(COC2=CC=CC(C3=CCN(CC3)CC4=NC5=C(N=C(C=C5)C(O)=O)N4C[C@H]6OCC6)=N2)C=CC(C7CC(F)(C7)F)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GLP-1R agonist 30 Related Classifications

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Help & FAQs
  • 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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