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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
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