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  4. Danuglipron tromethamine

Danuglipron tromethamine  (Synonyms: PF-06882961 tromethamine)

Cat. No.: HY-125824A
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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 No. : 2230198-03-3

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Danuglipron tromethamine Related Antibodies

Top Publications Citing Use of Products

    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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    Description

    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[1][2].

    In Vitro

    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.

    Danuglipron tromethamine Related Antibodies
    In Vivo

    Danuglipron (PF-06882961; 10 mg/kg; po; a single dose) tromethamine reduces blood glucose levels following intraperitoneal glucose tolerance test (IPGTT) in the hGLP-1R mouse model[2].
    Pharmacokinetic Parameters of Danuglipron in Male Wistar rats and Male cynomolgus monkeys[1].
    1.19

    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.

    Animal Model: C57BL/6 mice expressing humanized GLP-1R[2]
    Dosage: 10 mg/kg
    Administration: po; a single dose
    Result: Lowered blood glucose levels following IPGTT.
    Essai clinique
    Masse moléculaire

    676.73

    Formule

    C35H41FN6O7
    CAS No.
    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
    Livraison

    Room temperature in continental US; may vary elsewhere.
    Stockage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Pureté et documentation
    Références
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    Danuglipron tromethamine Related Classifications

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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Danuglipron2230198-03-3PF-06882961PF06882961PF 06882961GCGRGlucagon ReceptororallybioavailableGLP-1RT2DMDiabetesDiseaseInhibitorinhibitorinhibit

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