GIPR antagonist 4
GIPR antagonist 4 is an orally active GIPR antagonist with an IC50 of 4.1 nM. GIPR antagonist 4 exerts its antagonistic effect by competitively binding to GIPR and blocking the increase in Gαs-mediated cAMP production induced by GIP agonists. The combination of GIPR antagonist 4 and Liraglutide (HY-P0014) can enhance the weight loss effect of the single drug. GIPR antagonist 4 can be used for research related to obesity and metabolic diseases.
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- CAS No.: 3059496-70-4
- Formule: C28H29N3O4
- Masse moléculaire:471.55
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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GIPR 4.1 nM (IC50) |
GIPR antagonist 4 (0.1-40 μM; 2.5 h) showed GIPR antagonistic activity in CHO-K1 cells stably expressing the human GIPR receptor, with an IC50 of 4.1 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male hGIPR KI (C57Bl/6NTac background) mice, approximately 18-19 weeks old with a body weight of approximately 43-44 g, were fed a 60% high-fat diet for 12 weeks, after which dosing was initiated[1].
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Dosage:30 mg/kg
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Administration:po, once daily, 20 days
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Result:Resulted in a 17.1% greater reduction in body weight than the this compound monotherapy group, as measured by percent body weight change from baseline on Day 20. Resulted in a 3.9% greater reduction in body weight than the liraglutide monotherapy group, as measured by percent body weight change from baseline on Day 20.
Chemical Information
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CAS No. 3059496-70-4
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Masse moléculaire 471.55
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Formule C28H29N3O4
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SMILES
OC(C(C=C1)=CC=C1C(C=C2)=CC=C2NC([C@@H]3N(CCC3)C(NC4=CC=C(C(C)C)C=C4)=O)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GIPR antagonist 4 Related Classifications
HY-184966 Related Classifications
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- GIPR antagonist 4
- 3059496-70-4
- GIPR antagonist4
- GIPR antagonist-4
- Adhesion G Protein-coupled Receptors (AGPCRs)
- GIPR
- GIP receptor
- antagonist
- glucose-dependent insulinotropic polypeptide receptor
- obesity
- metabolic disease
- weight loss
- liraglutide
- combination therapy
- CHO-K1
- hGIPR
- cAMP
- HTRF
- high-fat diet
- hGIPR KI mouse
- BMI
- overweight
- small molecule
- Pfizer
- Inhibitor
- inhibitor
- inhibit