PF-07976016
Based on 1 Customer Validation
PF-07976016 (GIPR antagonist 4) is an orally active GIPR antagonist with an IC50 of 4.1 nM. PF-07976016 (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. PF-07976016 (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
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
GIPR 4.1 nM (IC50) |
In Vitro
PF-07976016 (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. Further protocols information, click here.
In Vivo
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
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (106.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.12 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Purity & Documentation
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Data Sheet (290 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
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.1207 mL | 10.6033 mL | 21.2067 mL | 53.0166 mL |
| 5 mM | 0.4241 mL | 2.1207 mL | 4.2413 mL | 10.6033 mL | |
| 10 mM | 0.2121 mL | 1.0603 mL | 2.1207 mL | 5.3017 mL | |
| 15 mM | 0.1414 mL | 0.7069 mL | 1.4138 mL | 3.5344 mL | |
| 20 mM | 0.1060 mL | 0.5302 mL | 1.0603 mL | 2.6508 mL | |
| 25 mM | 0.0848 mL | 0.4241 mL | 0.8483 mL | 2.1207 mL | |
| 30 mM | 0.0707 mL | 0.3534 mL | 0.7069 mL | 1.7672 mL | |
| 40 mM | 0.0530 mL | 0.2651 mL | 0.5302 mL | 1.3254 mL | |
| 50 mM | 0.0424 mL | 0.2121 mL | 0.4241 mL | 1.0603 mL | |
| 60 mM | 0.0353 mL | 0.1767 mL | 0.3534 mL | 0.8836 mL | |
| 80 mM | 0.0265 mL | 0.1325 mL | 0.2651 mL | 0.6627 mL | |
| 100 mM | 0.0212 mL | 0.1060 mL | 0.2121 mL | 0.5302 mL |
PF-07976016 Related Classifications
HY-184966 Related Classifications
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Keywords
- 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