GCGR-IN-17( PF-06291874 | PF06291874 | PF-6291874 )

Catalog No. M11636 CAS No. 1393124-08-7

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

GCGR-IN-17
Note

Research use only, not for human use.
Brief Description

A highly potent glucagon receptor antagonist with Ki of 14 nM for hGCGR.
Description

A highly potent glucagon receptor antagonist with Ki of 14 nM for hGCGR; shows excellent selectivity against a panel of 69 receptors, ion channels, uptake sites and enzymes; reduces the glucagon-elicited glucose excursion in a dose-dep endent manner in rats; displays low in vivo clearance and excellent oral bioavailability in both rats and dogs.Diabetes Phase 2 Discontinued.
In Vitro

——
In Vivo

PF-06291874 exposure is approximately dose-proportional with a half-life of ～19.7-22.7 h. PF-06291874 has a fast on and off rate. PF-06291874 is highly bound to human plasma protein, with a mean free fraction of ～0.55%.
Synonyms

PF-06291874 | PF06291874 | PF-6291874
Pathway

GPCR/G Protein
Target

Glucagon Receptor
Recptor

Glucagon Receptor
Research Area

Metabolic Disease
Indication

Diabetes

CAS Number

1393124-08-7
Formula Weight

503.5134
Molecular Formula

C26H28F3N3O4
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 30 mg/mL
SMILES

O=C(O)CCNC(C1=CC=C([C@@H](OC2=CC(C)=C(C(C)=C2)N3C=C(C=N3)C(F)(F)F)CCC)C=C1)=O
Chemical Name

glucagon receptor antagonists-4, N-[4-[(1S)-1-[3,5-dimethyl-4-[4-(trifluoromethyl)-1H-pyrazol-1-yl]phenoxy]butyl]benzoyl]-

1. Guzman-Perez A, et la. Bioorg Med Chem Lett. 2013 May 15;23(10):3051-8.

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