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APD 668

Names

[ CAS No. ]:
832714-46-2

[ Name ]:
APD 668

[Synonym ]:
Isopropyl 4-({1-[2-fluoro-4-(methylsulfonyl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-4-yl}oxy)-1-piperidinecarboxylate
1-Piperidinecarboxylic acid, 4-[[1-[2-fluoro-4-(methylsulfonyl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-4-yl]oxy]-, 1-methylethyl ester
APD 668
APD668

Biological Activity

[Description]:

APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively..IC50 value: 2.7 nM (EC50) [1]Target: GPR119Chronic treatment withAPD668 showed for the first time that blood glucose and glycated hemoglobin (HbA1c) levels could be significantly reduced in Zucker Diabetic Fatty (ZDF) rats over several weeks of dosing. APD668 was the ?rst compound with thismechanism of action to be progressed into clinical development for the treatment of diabetes.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> GPR119
Research Areas >> Metabolic Disease

[References]

[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.


[Related Small Molecules]

AR 231453 | MBX-2982 | JNJ-38431055 | PSN632408 | GSK1292263 | Firuglipel

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
611.6±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C21H24FN5O5S

[ Molecular Weight ]:
477.509

[ Flash Point ]:
323.7±31.5 °C

[ Exact Mass ]:
477.148224

[ PSA ]:
124.89000

[ LogP ]:
1.99

[ Appearance of Characters ]:
white solid

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.658

[ Storage condition ]:
-20℃

Related Compounds