1. GPCR/G Protein
  2. GLP Receptor
  3. GLP-1 receptor agonist 22

GLP-1 receptor agonist 22 is an orally active GLP-1 receptor agonist. GLP-1 receptor agonist 22 promotes the accumulation of cAMP. GLP-1 receptor agonist 22 reduces blood glucose levels and inhibits feeding behavior in human glucagon-like peptide-1 receptor knock-in mice. GLP-1 receptor agonist 22 can be used in the research of type 2 diabetes and obesity.

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GLP-1 receptor agonist 22

GLP-1 receptor agonist 22 Chemical Structure

CAS No. : 3124217-40-6

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Description

GLP-1 receptor agonist 22 is an orally active GLP-1 receptor agonist. GLP-1 receptor agonist 22 promotes the accumulation of cAMP. GLP-1 receptor agonist 22 reduces blood glucose levels and inhibits feeding behavior in human glucagon-like peptide-1 receptor knock-in mice. GLP-1 receptor agonist 22 can be used in the research of type 2 diabetes and obesity[1].

IC50 & Target[1]

GLP-1

 

In Vitro

GLP-1 receptor agonist 22 (24-P1) potently agonizes hGLP-1R in HEK293 cells stably expressing hGLP-1R with an EC50 of 0.53 nM[1].
GLP-1 receptor agonist 22 (24-P1) has enhanced permeability in Caco-2 cells, with an apical-to-basal apparent permeability of 4.75 nm/s and an efflux ratio of 2.11[1].

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

Parmacokinetics
Species Dose Route Cmax AUC0-24 CL Tmax T1/2 Bioavailability
Mice[1] 1.0 mg/kg i.v. 520 ng/mL 3472 ng·h/mL 4.5 mL/min/kg / / /
Mice[1] 10 mg/kg p.o. 4657 ng/mL 25137 ng·h/mL / 1.00 h 3.52 h 72.4 %
In Vivo

GLP-1 receptor agonist 22 (0.03-3 mg/kg; p.o.; single administration) dose-dependently reduces blood glucose levels and improves glucose tolerance in hGLP-1R knock-in mice. At an oral dose of 3 mg/kg, it significantly inhibits cumulative food intake in hGLP-1R knock-in mice, exhibiting potent early-stage effects[1].

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

Animal Model: hGLP-1R knock-in mice[1]
Dosage: 0.03 mg/kg; 0.1 mg/kg/3 mg/kg
Administration: p.o.; single dose
Result: Significantly reduced blood glucose levels relative to vehicle at both 0.03 mg/kg and 0.1 mg/kg doses.
Lowered the area under the curve (AUC0-90ₘᵢₙ) for glucose levels significantly compared to vehicle.
Markedly suppressed cumulative food consumption at 3 mg/kg, with a strong early inhibitory effect observed at 3-6 h postdose relative to vehicle.
Significantly reduced cumulative food intake at 24 h postdose, with the inhibitory effect gradually converging with that of Orforglipron (HY-112185).
Molecular Weight

896.02

Formula

C50H54FN9O6

CAS No.
SMILES

CC1=C(C(C)=CC(N2N=C3CCN([C@H](C3=C2N4C=CN(C4=O)C5=CC6=C(CN(CCO6)C)C=C5)C)C(C7=CC8=C(N7[C@@]9([C@@H](C)C9)C%10=NOC(N%10)=O)C=CC([C@H]%11CCOC(C)(C%11)C)=C8)=O)=C1)F

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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.

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Product Name:
GLP-1 receptor agonist 22
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HY-183694
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