Firuglipel (DS8500, DS8500a)

Chemical Structure : Firuglipel

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货号: PC-60042Not For Human Use, Lab Use Only.

Firuglipel (DS8500, DS8500a) is a novel potent, selective, orally available GPR119 agonist with EC50 of 51.5 nM in human GPR119-expressing CHO-K1 cells.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

Firuglipel (DS8500, DS8500a) is a novel potent, selective, orally available GPR119 agonist with EC50 of 51.5 nM in human GPR119-expressing CHO-K1 cells.
Firuglipel displays no significant effect on 66 receptors, channels, or transporters.
Firuglipel enhances glucose-stimulated insulin secretion in Sprague-Dawley rats and promotes GLP-1 secretion in Zucker fatty rats, preserved β cell function and prevented increases in glycohemoglobin concentrations in rodent models of type 2 diabetes.

物理化学性质&存储条件

分子量	467.497
分子式	C25H26FN3O5
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
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Solubility	10 mM in DMSO
Chemical Name/SMILES	4-(5-{(1R)-1-[4-(cyclopropanecarbonyl)phenoxy]propyl}-1,2,4-oxadiazol-3-yl)-2-fluoro-N-[(2R)-1-hydroxypropan-2-yl]benzamide

参考文献

1. Patent WO2012050151.

2. Inagaki N, et al. BMJ Open Diabetes Res Care. 2017 Sep 29;5(1):e000424.

3. Terauchi Y, et al. J Diabetes Investig. 2018 Apr 1. doi: 10.1111/jdi.12846.

4. Makino C, et al. Xenobiotica. 2018 Aug 20:1-33. doi: 10.1080/00498254.2018.1514545.