2. GPCR/G Protein
  3. GLP Receptor
  4. 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.

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GLP-1 receptor agonist 21

GLP-1 receptor agonist 21 Chemical Structure

CAS No. : 3124217-54-2

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GLP-1 receptor agonist 21 Related Antibodies

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Description

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[1].

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.

GLP-1 receptor agonist 21 Related Antibodies
Parmacokinetics
Species Dose Route Cmax AUC0-24 CL Tmax T1/2 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 (AUC0-90 min) relative to vehicle at 0.03 mg/kg.
Dose-dependently improved glucose tolerance and significantly reduced blood glucose AUC0-90 min relative to vehicle at 0.1 mg/kg.
Molecular Weight

908.99

Formula

C50H50F2N10O5
CAS No.
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
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References
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GLP-1 receptor agonist 21 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-1 receptor agonist 213124217-54-2GLP ReceptorhGLP-1R knock-in micecAMPhuman liver microsomesobesityblood glucose levelstype 2 diabetes mellitushGLP-1Rhuman glucagon-like peptide-1 receptorCaco-2 cellsHEK293 cellsInhibitorinhibitorinhibit

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