Danuglipron tromethamine
Based on 4 publication(s) in Google Scholar
Danuglipron (PF-06882961) tromethamine is an orally active glucagon-like peptide-1 receptor (GLP-1R) agonist. Danuglipron tromethamine has the potential for type 2 diabetes research.
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- CAS 番号: 2230198-03-3
- 分子式: C35H41FN6O7
- 分子量:676.73
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
MedChemExpress(MCE)の使用を引用している文献 Danuglipron tromethamine
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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
生物活性
Danuglipron (PF-06882961) tromethamine shows agonist activities at both the cAMP and βArr pathways. Danuglipron tromethamine 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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2230198-03-3
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分子量 676.73
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分子式 C35H41FN6O7
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SMILES
OCC(CO)(N)CO.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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別名
PF-06882961 tromethamine
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
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 tromethamine 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 tromethamine 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 tromethamine 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 tromethamine 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 tromethamine 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 tromethamine 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 -
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)