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AMG151 HCl

Product Specifications

CAS Number

1609674-80-7

Target

Others

Related Pathways

Others

Bioactivity

ARRY-403, also known as AMG-151, is an orally available allosteric glucokinase (GK) activator developed for the treatment of type 2 diabetes mellitus (T2DM) . ARRY-403 has many favorable physicochemical characteristics and ADME properties (low potential to cause drug–drug interactions (DDIs) . ARRY-403 potently activates human glucokinase (GK) in vitro (EC50 = 79 nM at 5 mM glucose), with an S0.5 = 0.93 mM glucose (ARRY-403 at 5 mM) and Vmax = 134% compared to the no activator control. It possesses good in vitro drug-like properties (aqueous solubility, cell permeability, low low potential for drug-drug interactions, low predicted hepatic clearance), and selectivity against broad panels of receptors and enzymes.

Smiles

Cl.Cl.Cc1ncccc1Oc1cc(Sc2ccccn2)cnc1Nc1nc(ns1)[C@H](O)CO

Molecular Formula

C20H20Cl2N6O3S2

Molecular Weight

527.439

Shipping Conditions

Ice Packs

Storage Temperature

-20°C

Available Sizes

Frequently Asked Questions

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