PF-06291874 is an orally active, potent and selective glucagon receptor antagonist. PF-06291874 exhibits a robust glucose reductions in subjects with type 2 diabetes mellitus.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO: 15 mg/mL|
Identification of a novel conformationally constrained glucagon receptor antagonist.
Lee EC, et al. Bioorg Med Chem Lett. 2014 Feb 1;24(3):839-44. PMID: 24418771.
The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus.
Guzman-Perez A, et al. Bioorg Med Chem Lett. 2013 May 15;23(10):3051-8. PMID: 23562063.
|Related Glucagon Receptor Products|
PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor (GLP-1R) agonist.
Teduglutide is a glucagon-like peptide-2 (GLP- 2) receptor agonist used for the treatment of short-bowel syndrome.
NNC0640 is a potent, negative allosteric modulator (NAM) of human G-protein-coupled glucagon receptor (GCGR) with IC50 of 69.2 nM.
|Avexitide (Exendin 9-39)
Avexitide (Exendin 9-39) is a specific and competitive GLP-1 receptor antagonist.
Cotadutide acetate is a potent peptide dual agonist of glucagon-like peptide-1 (GLP-1) and glucagon receptor, with EC50 values of 6.9 pM and 10.2 pM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.