Danuglipron
Based on 4 publication(s) in Google Scholar
Danuglipron (PF-06882961) is an orally active glucagon-like peptide-1 receptor (GLP-1R) agonist. Danuglipron has the potential for type 2 diabetes research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.85%
- CAS. Nr.: 2230198-02-2
- Formel: C31H30FN5O4
- Molecular Weight:555.60
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Speicherung:Powder -20°C, 3 years , 4°C, 2 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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Danuglipron
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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IF
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RT-PCR
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In Vivo Efficacy Study
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In Vivo Efficacy Study
Biologische Aktivität
Beschreibung
IC50 & Target
In Vitro
Danuglipron (PF-06882961) shows agonist activities at both the cAMP and βArr pathways. Danuglipron is a full agonist (EC50 of 13 nM) in the CS cAMP assay. Danuglipron is a partial agonist in recruiting βArr2 (EC50 of 490 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Pharmacokinetic Parameters of Danuglipron in Male Wistar rats and Male cynomolgus monkeys[1].
| Species | Dose (mg/kg) | Cmax (ng/mL) | Tmax (h) | AUC0–∞ (ng h/mL) | CLp (mL/min/kg) | Vdss (L/kg) | t1/2 (h) | Oral F (%) |
| rat | 1.0 (iv) | - | - | 296 ± 39.8 | 57.3 ± 8.68 | 0.86 ± 0.38 | 1.13 ± 0.84 | - |
| rat | 5.0 (po) | 141 | 0.5 | 168 | - | - | 0.63 | 11 |
| rat | 100 (po) | 2820 | 0.75 | 11900 | - | - | 2.37 | 39 |
| monkey | 1.0 (iv) | - | - | 1240 | 13.8 | 0.266 | 1.89 | - |
| monkey | 5.0 (po) | 68.7 | 1.5 | 303 | - | - | 6.92 | 5.0 |
| monkey | 100 (po) | 1150 ± 715 | 3.3 ± 2.5 | 11000 ± 3500 | - | - | 6.37 | 9.0 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice expressing humanized GLP-1R[2]
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Dosage:10 mg/kg
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Administration:po; a single dose
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Result:Lowered blood glucose levels following IPGTT.
Chemical Information
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CAS. Nr. 2230198-02-2
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Appearance Solid
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Molecular Weight 555.60
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Formel C31H30FN5O4
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Color White to light yellow
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SMILES
FC(C=C(C=C1)C#N)=C1COC2=NC(C(CC3)CCN3CC(N(C4=C5)C[C@@H]6CCO6)=NC4=CC=C5C(O)=O)=CC=C2
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Synonyms
PF-06882961
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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J Cell Mol Med
Danuglipron Ameliorates Pressure Overload-Induced Cardiac Remodelling Through the AMPK Pathway. [Abstract]2025 Mar;29(5):e70488. PMID: 40070049
Danuglipron purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2025 Mar;29(5):e70488. [Abstract]
(A) NRCMs were treated with different concentrations of Danuglipron (PF; 0, 0.05, 0.1, 0.3, 0.9, and 1.2μg/mL) for 24 h, and cell viability was assessed to determine the dose-dependent effects of PF on cardiomyocyte survival. (B) NRCMs were treated with 0.1μg/mL PF for 0, 12, 24, 48, 72, and 96h, followed by the assessment of cell viability at each time point.
Danuglipron purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2025 Mar;29(5):e70488. [Abstract]
Neonatal rat cardiomyocytes (NRCMs) were treated with 100 μM PE for 24–48 h to induce hypertrophy, with or without co‐treatment with Danuglipron (PF) at the previously determined optimal concentration of 0.1 μg/mL. Representative immunofluorescence images of NRCMs stained for α-actinin (red) under different treatment conditions: PBS (control), PF alone, PE alone, and PE+PF.
Danuglipron purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2025 Mar;29(5):e70488. [Abstract]
Neonatal rat cardiomyocytes (NRCMs) were treated with 100 μM PE for 24–48 h to induce hypertrophy, with or without co‐treatment with Danuglipron (PF) at the previously determined optimal concentration of 0.1 μg/mL. Relative mRNA expression levels of hypertrophy-related markers (ANP, BNP, and β-MHC) in NRCMs under different treatment conditions, as determined by RT-PCR.
Danuglipron purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2025 Mar;29(5):e70488. [Abstract]
Danuglipron (PF; 1, 3, 9 mg/kg; po; daily for 8 weeks was initiated 3 days after AB surgery) in C57BL/6 mice using aortic banding (AB) surgery. Representative M-mode echocardiographic images of left ventricular function in different treatment groups.
Danuglipron purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2025 Mar;29(5):e70488. [Abstract]
Danuglipron (PF; 1, 3, 9 mg/kg; po; daily for 8 weeks was initiated 3 days after AB surgery) in C57BL/6 mice using aortic banding (AB) surgery revealed that hearts from AB mice were significantly enlarged, with hypertrophic cardiomyocytes compared to the sham group. Representative images of gross morphology of mouse hearts (A), (B) H&E-stained cross-sections of the hearts.
Danuglipron purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2025 Mar;29(5):e70488. [Abstract]
Danuglipron (PF; 1, 3, 9 mg/kg; po; daily for 8 weeks was initiated 3 days after AB surgery) in C57BL/6 mice using aortic banding (AB) surgery treatment dose‐dependently increased p‐AMPKα levels in AB mice, with the low dose showing the most pronounced effect. Representative western blot images showing the expression of p-AMPKα, AMPKα, and HSP70 in heart tissues from C57BL/6 mice across different treatment groups. GAPDH serves as a loading control.
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Expert Opin Emerg Drugs
2021 Sep;26(3):231-243. PMID: 34176426 -
J Pharm Biomed Anal
Comprehensive identification and characterization of in vitro and in vivo metabolites of the novel GLP-1 receptor agonist danuglipron using UHPLC-QToF-MS/MS. [Abstract]2026 Jan 1:267:117128. PMID: 40865303 -
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (179.99 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protokoll
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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
Reinheit & Dokumentation
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Data Sheet (276 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)
Verweise
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 | 1.7999 mL | 8.9993 mL | 17.9986 mL | 44.9964 mL |
| 5 mM | 0.3600 mL | 1.7999 mL | 3.5997 mL | 8.9993 mL | |
| 10 mM | 0.1800 mL | 0.8999 mL | 1.7999 mL | 4.4996 mL | |
| 15 mM | 0.1200 mL | 0.6000 mL | 1.1999 mL | 2.9998 mL | |
| 20 mM | 0.0900 mL | 0.4500 mL | 0.8999 mL | 2.2498 mL | |
| 25 mM | 0.0720 mL | 0.3600 mL | 0.7199 mL | 1.7999 mL | |
| 30 mM | 0.0600 mL | 0.3000 mL | 0.6000 mL | 1.4999 mL | |
| 40 mM | 0.0450 mL | 0.2250 mL | 0.4500 mL | 1.1249 mL | |
| 50 mM | 0.0360 mL | 0.1800 mL | 0.3600 mL | 0.8999 mL | |
| 60 mM | 0.0300 mL | 0.1500 mL | 0.3000 mL | 0.7499 mL | |
| 80 mM | 0.0225 mL | 0.1125 mL | 0.2250 mL | 0.5625 mL | |
| 100 mM | 0.0180 mL | 0.0900 mL | 0.1800 mL | 0.4500 mL |
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