PF-06882961

PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor agonist (GLP-1R).

Product information

CAS Number: 2230198-02-2

Molecular Weight: 555.60

Formula: C31H30FN5O4

Chemical Name: (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-carboxylic acid

Smiles: N#CC1=CC(F)=C(COC2=CC=CC(=N2)C2CCN(CC3=NC4=CC=C(C=C4N3C[C@@H]3CCO3)C(O)=O)CC2)C=C1

InChiKey: HYBAKUMPISVZQP-DEOSSOPVSA-N

InChi: InChI=1S/C31H30FN5O4/c32-25-14-20(16-33)4-5-23(25)19-41-30-3-1-2-26(35-30)21-8-11-36(12-9-21)18-29-34-27-7-6-22(31(38)39)15-28(27)37(29)17-24-10-13-40-24/h1-7,14-15,21,24H,8-13,17-19H2,(H,38,39)/t24-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 100 mg/mL(179.98 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

PF-06882961 stimulates cAMP accumulation in CHO cells expressing both the human and monkey GLP-1Rs with comparable EC50 values. In contrast, PF-06882961 does not increase cAMP levels in cells expressing the mouse, rat, or rabbit GLP-1R.

In Vivo:

PF-06882961 potentiates glucose-stimulated insulin release and reduces food intake in monkeys.

References:

1. Griffith DA, et al. bioRxiv. 2020 Sep 30.
2. Hun Jee Choe, Young Min Cho. Endocrinol Metab (Seoul). 2021 Feb;36(1):22-29.

Products are for research use only. Not for human use.