APD668 (JNJ-28630368) | GPR119 agonist | Probechem Biochemicals

Chemical Structure : APD668

CAS No.: 832714-46-2

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APD668 (APD 668, JNJ-28630368)

货号: 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.

规格	价格	库存
5 mg	￥1180	In stock
10 mg	￥1880	In stock
25 mg	￥2980	In stock
50 mg	￥4880	In stock
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	477.51
分子式	C21H24FN5O5S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-Methylethyl 4-[[1-[2-fluoro-4-(methylsulfonyl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-4-yl]oxy]-1-piperidinecarboxylate

参考文献

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.

APD668 (APD 668, JNJ-28630368)

生物&药学活性

物理化学性质&存储条件

参考文献

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APD668 (APD 668, JNJ-28630368)

生物&药学活性

物理化学性质&存储条件

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