APD668

APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM) . APD668 can be used for the research of steatohepatitis and diabetes[1][2].

Product Specifications

CAS Number

[832714-46-2]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Cytochrome P450; GPR119; Potassium Channel

Type

Reference compound

Related Pathways

GPCR/G Protein; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/APD668.html

Purity

99.73

Solubility

DMSO : 33.33 mg/mL (ultrasonic)

Smiles

O=C(OC(C)C)N(CC1)CCC1OC2=C3C(N(C4=CC=C(S(=O)(C)=O)C=C4F)N=C3)=NC=N2

Molecular Formula

C21H24FN5O5S

Molecular Weight

477.51

Precautions

H315, H319, H335

References & Citations

[1]Semple G, et al. Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control. Bioorg Med Chem Lett. 2011 May 15;21 (10) :3134-41.|[2]Bahirat UA, et, al. APD668, a G protein-coupled receptor 119 agonist improves fat tolerance and attenuates fatty liver in high-trans fat diet induced steatohepatitis model in C57BL/6 mice. Eur J Pharmacol. 2017 Apr 15;801:35-45.