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

Product 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 No.: 2230198-03-3
Chemical 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
Synonyms: PF-06882961-82;UNII-2HJV78O0SS;Danuglipron tromethamine;PF-06882961 tromethamine;PF 06882961 Tris,PF06882961 Tris;2-[[4-[6-[(4-cyano-2-fluoro-phenyl)methoxy]-2-pyridyl]-1-piperidyl]methyl]-3-[[(2S)-oxetan-2-yl]methyl]benzimidazole-5-carboxylic acid;2-amino-2-(hydroxymethyl)propane-1,3-diol 2-[[4-[6-[(4-cyano-2-fluoro-phenyl)methoxy]-2-pyridyl]-1-piperidyl]methyl]-3-[[(2S)-oxetan-2-yl]methyl]benzimidazole-5-carboxylic acid;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
CBNumber: CB55856377
Molecular Formula: C35H41FN6O7
Formula Weight: 676.75
MOL File: 2230198-03-3.mol

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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 Property

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|

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Hazard and Precautionary Statements (GHS)

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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 Chemical Properties,Usage,Production

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)	C_max (ng/mL)	T_max (h)	AUC_0–∞ (ng h/mL)	CL_p (mL/min/kg)	Vd_ss (L/kg)	t_1/2 (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.

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 Preparation Products And Raw materials

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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 Suppliers

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2230198-03-3, 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-carboxylateRelated Search:

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

PF-06882961-82

Danuglipron tromethamine

UNII-2HJV78O0SS

PF-06882961 tromethamine

PF 06882961 Tris,PF06882961 Tris

2-[[4-[6-[(4-cyano-2-fluoro-phenyl)methoxy]-2-pyridyl]-1-piperidyl]methyl]-3-[[(2S)-oxetan-2-yl]methyl]benzimidazole-5-carboxylic acid

2-amino-2-(hydroxymethyl)propane-1,3-diol 2-[[4-[6-[(4-cyano-2-fluoro-phenyl)methoxy]-2-pyridyl]-1-piperidyl]methyl]-3-[[(2S)-oxetan-2-yl]methyl]benzimidazole-5-carboxylic acid

2230198-03-3