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Chemical Structure : APD668
CAS No.: 832714-46-2
Catalog No.: PC-20437Not For Human Use, Lab Use Only.
APD668 (JNJ-28630368) is a potent and selective GPR119 agonist with EC50 of 2.7 and 33 nM for huamn and rat GPR119, respectively.
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|---|---|---|---|
| 25 mg | $258 | In stock | |
| 100 mg | $598 | In stock | |
| 200 mg | $898 | In stock | |
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APD668 (JNJ-28630368) is a potent and selective GPR119 agonist with EC50 of 2.7 and 33 nM for huamn and rat GPR119, respectively.
APD668 increases adenylate cyclase activation in HEK293 cells transfected with human GPR119 with EC50 of 23 nM.
APD668 enhances insulin release from both rat and human isolated pancreatic islets in a glucose-dependent manner.
APD668 does not show any binding in a panel of 80 known receptors and ion channels.
APD668 displays no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki = 0.1 uM).
APD668 (30 mg/kg) significantly reduced blood glucose and glycated hemoglobin (HbA1c) levels over eight weeks of treatment (QD), with no desensitization of the acute drug response in Zucker Diabetic Fatty (ZDF) rats.
| M.Wt | 477.51 | |
| Formula | C21H24FN5O5S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
1-Methylethyl 4-[[1-[2-fluoro-4-(methylsulfonyl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-4-yl]oxy]-1-piperidinecarboxylate |
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1. Semple G, et al. Bioorg Med Chem Lett. 2011 May 15;21(10):3134-41.
2. Bahirat UA, et al. Eur J Pharmacol. 2017 Apr 15;801:35-45.
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