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Cat. No.: HY-183693

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GLP-1 receptor agonist 21

GLP-1 receptor agonist 21 is an orally active glucagon-like peptide-1 receptor (GLP-1R) agonist with an EC₅₀ of 0.64 nM. GLP-1 receptor agonist 21 reduces blood glucose levels and suppresses cumulative food consumption in diabetic mice. GLP-1 receptor agonist 21 can be used for the researches of type 2 diabetes and obesity.

For research use only. We do not sell to patients.

CAS No.: 3124217-54-2
Formula: C₅₀H₅₀F₂N₁₀O₅
Molecular Weight:908.99

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

GLP-1 receptor agonist 21 Chemical Structure

CAS No.: 3124217-54-2

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

hGLP-1R

0.64 μM (EC₅₀)

In Vitro

GLP-1 receptor agonist 21 (Compound 17-P1) potently activates hGLP-1R in stably transfected HEK293 cells with an EC₅₀ of 0.64 nM^[1].
GLP-1 receptor agonist 21 exhibits favorable metabolic stability in human liver microsomes and has enhanced permeability in Caco-2 cells^[1].

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

Parmacokinetics

Species	Dose	Route	C_max	AUC_0-24	CL	T_max	T_1/2	F
Mice^[1]	1.0 mg/kg	i.v.	1220 ng/mL	9338 ng·h/mL	1.8 mL/min/kg	/	/	/
Mice^[1]	10 mg/kg	p.o.	13333 ng/mL	50415 ng·h/mL	/	0.83 h	2.84 h	54.0 %

In Vivo

GLP-1 receptor agonist 21 (Compound 17-P1) (0.03-0.1 mg/kg; p.o.; single dose) dose-dependently improves glucose tolerance in hGLP-1R knock-in mice, with significant reductions in blood glucose^[1].
17-P1 (3 mg/kg; p.o.; single dose) significantly suppresses cumulative food intake in hGLP-1R knock-in mice for 24 hours^[1].

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

Animal Model:

Type 2 diabetic hGLP-1R knock-in mice^[1]
Dosage:

0.03 mg/kg; 0.1 mg/kg
Administration:

p.o.; single dose
Result:

Significantly reduced blood glucose area under the curve (AUC_0-90 min) relative to vehicle at 0.03 mg/kg.
Dose-dependently improved glucose tolerance and significantly reduced blood glucose AUC_0-90 min relative to vehicle at 0.1 mg/kg.

Chemical Information

CAS No. 3124217-54-2
Molecular Weight 908.99
Formula C₅₀H₅₀F₂N₁₀O₅
SMILES

CC1=C(C(C)=CC(N2N=C3CCN([C@H](C3=C2N4C=CN(C4=O)C5=C(C6=C(N=C7CCCN76)C=C5)F)C)C(C8=CC9=C(N8[C@@]%10([C@@H](C)C%10)C%11=NOC(N%11)=O)C=CC([C@H]%12CCOC(C)(C%12)C)=C9)=O)=C1)F
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

Handling Instructions (2659 KB)

References

[1]. Li, Mengya, et al. Discovery of Small-Molecule GLP-1 Receptor Agonists with Improved Oral Pharmacokinetics Based on Orforglipron. ACS Medicinal Chemistry Letters (2026).

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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