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APD668

Cat. No. M3950

All AbMole products are for research use only, cannot be used for human consumption.

APD668 Structure
Size Price Availability Quantity
10mM*1mL in DMSO USD 135  USD135 In stock
5mg USD 119  USD119 In stock
10mg USD 198  USD198 In stock
25mg USD 390  USD390 In stock
50mg USD 580  USD580 In stock
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Quality Control & Documentation
Biological Activity

APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively. APD668 pairs are divided by CYP2C9 (KiNone of the five major CYP subtypes other than =0.1 μM) had no significant inhibitory effect. APD668 can be used for research on steatohepatitis and diabetes. ADP668 showed activity to reduce blood glucose and glycated hemoglobin (HbA1c) levels in Zucker Diabetic Fatty (ZDF) rats over several weeks of dosing. APD668 significantly improved blood glucose handling during glucose challenge in several diabetic and non-diabetic rodent models, showing a clear glucose-dependent effect on insulin release in a hyperglycemic clamp model in the Sprague–Dawley rat. APD668 is not genotoxic, and shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki value 0.1 μM).

Chemical Information
Molecular Weight 477.51
Formula C21H24FN5O5S
CAS Number 832714-46-2
Form Solid
Solubility (25°C) DMSO 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Sakairi M, et al. Chem Pharm Bull (Tokyo) Synthesis and pharmacological profile of a new selective G protein-coupled receptor 119 agonist; 6-((2-fluoro-3-(1-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-4-yl)propyl)amino)-2,3-dihydro-1H-inden-1-one.

[2] Semple G, et al. Bioorg Med Chem Lett. Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.

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Keywords: APD668 supplier, GPR/FFAR, inhibitors, activators

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