2. GPCR/G Protein
  3. GCGR
  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.

For research use only. We do not sell to patients.

Danuglipron tromethamine Chemical Structure

Danuglipron tromethamine Chemical Structure

CAS No. : 2230198-03-3

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Danuglipron tromethamine Related Antibodies

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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.
Molecular Weight

676.73

Formula

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
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Danuglipron tromethamine Related Classifications

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  • Do most proteins show cross-species activity?

    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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