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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- CAS No.: 3108380-54-4
- Formula: C33H32F3N5O4
- Molecular Weight:619.63
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
0.048 nM
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.
| Species | Dose | Route | T1/2 | Tmax | Plasma Concentration | AUC | Bioavailability | Clearance (CL) |
|---|---|---|---|---|---|---|---|---|
| Rat | 5 mg/kg | p.o. | 3.32 h | 2.67 h | 256.40 ng/mL | 1377.38 ng·h/mL | 54.25 % | 65.85 mL/min/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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].
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Dosage:1, 10 mg/kg
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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)
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Result:Dose-dependently decreased blood glucose level and increased glucose-stimulated insulin secretion in hGLP-1R knock-in mice.
Chemical Information
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CAS No. 3108380-54-4
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Molecular Weight 619.63
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Formula C33H32F3N5O4
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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