Danuglipron tromethamine
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.
- CAS No.: 2230198-03-3
- Formula: C35H41FN6O7
- Molecular Weight:676.73
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Semaglutide (crude)Crude Semaglutide
Biological Activity
Description
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.
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2230198-03-3
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Molecular Weight 676.73
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Formula 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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Synonyms
PF-06882961 tromethamine
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Danuglipron tromethamine Related Classifications
HY-125824A Related Classifications
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