PF-06291874

PF-06291874 is a highly potent, non-peptide and orally active glucagon receptor antagonist. PF-06291874 is under the study for type 2 diabetes mellitus (T2DM) [1][2].

Product Specifications

CAS Number

[1393124-08-7]

Product Name Alternative

Glucagon receptor antagonists-4

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

GCGR

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/glucagon-receptor-antagonists-4.html

Purity

99.31

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CCC[C@H](OC1=CC(C)=C(N2C=C(C(F)(F)F)C=N2)C(C)=C1)C3=CC=C(C(NCCC(O)=O)=O)C=C3

Molecular Formula

C26H28F3N3O4

Molecular Weight

503.51

Precautions

H302, H315, H319, H335

References & Citations

[1]Esther C.Y. Lee et al. Identification of a novel conformationally constrained glucagon receptor antagonist. Bioorg Med Chem Lett, 2014 Feb 1, 24 (3) :839-44.|[2]Derek J Nunez, et al. Glucagon receptor as a drug target: A witches' brew of eye of newt (peptides) and toe of frog (receptors) . Diabetes Obes Metab. 2018 Feb;20 (2) :233-237.|[3]D J Kazierad, et al. Effects of multiple ascending doses of the glucagon receptor antagonist PF-06291874 in patients with type 2 diabetes mellitus. Diabetes Obes Metab. 2016 Aug;18 (8) :795-802.