| Identification | Back Directory | [Name]
2-amino-2-(hydroxymethyl)propane-1,3-diol (S)-2-((4-(6-((4-cyano-2-fluorobenzyl)oxy)pyridin-2-yl)piperidin-1-yl)methyl)-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylate | [CAS]
2230198-03-3 | [Synonyms]
PF-06882961-82
UNII-2HJV78O0SS
PF-06882961 tromethamine
Danuglipron tromethamine
2-amino-2-(hydroxymethyl)propane-1,3-diol (S)-2-((4-(6-((4-cyano-2-fluorobenzyl)oxy)pyridin-2-yl)piperidin-1-yl)methyl)-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylate | [Molecular Formula]
C35H41FN6O7 | [MDL Number]
MFCD33029308 | [MOL File]
2230198-03-3.mol | [Molecular Weight]
676.75 |
| Chemical Properties | Back Directory | [InChIKey]
JEJPAGACGZQFHN-NETKZVBLNA-N | [SMILES]
C(N)(CO)(CO)CO.C([C@H]1OCC1)N1C(=NC2=CC=C(C(=O)O)C=C12)CN1CCC(C2=CC=CC(OCC3C=CC(C#N)=CC=3F)=N2)CC1 |&1:9,r| |
| Hazard Information | Back Directory | [Uses]
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 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 |
| 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. |
| [References]
[1] David A Griffithm, et al. A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor. J Med Chem. 2022 Jun 23;65(12):8208-8226. DOI:10.1021/acs.jmedchem.1c01856
[2] W. GUO, et al. Preclinical pharmacology of low molecular weight GLP-1 receptor agonist XW014. |
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