PF-07976016
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 98.08%
- CAS No.: 3059496-70-4
- Formula: C28H29N3O4
- Molecular Weight:471.55
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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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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Appearance Solid
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Molecular Weight 471.55
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Formula C28H29N3O4
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Color White to off-white
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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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Synonyms
GIPR antagonist 4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
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Data Sheet (287 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PF-07976016 Related Classifications
HY-184966 Related Classifications
Powered by Bioz
- PF-07976016
- 3059496-70-4
- GIPR antagonist 4
- PF07976016
- PF 07976016
- 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