GLPG0974
目录号: PL03046 纯度: ≥98%
CAS No. :1391076-61-1
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中文名称
GLPG0974
中文别名
GLPG-0974
英文名称
GLPG0974
英文别名
GLPG-0974;GLPG0974
Cas No.
1391076-61-1
分子式
C25H25N2O4Scl
分子量
485.00
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
GLPG0974是游离脂肪酸受体-2 (free fatty acid receptor-2 (FFA2/GPR43)) 拮抗剂,IC50 值为 9 nM。
生物活性
GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC 50 of 9 nM.
性状
Solid
IC50 & Target[1][2]
IC50: 9 nM (GPR43)
体外研究(In Vitro)
GLPG0974 is able to inhibit acetate-induced neutrophil migration strongly in vitro and demonstrates ability to inhibit a neutrophil-based pharmacodynamic (PD) marker, CD11b activation-specific epitope [AE], in a human whole blood assay. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
GLPG0974 shows excellent pharmacokinetic properties in rat with a bioavailability of 47% and a linear increase of the plasma exposure after oral dosing at 5 and 30 mg/kg. The extended half-life observed following the increase of oral dose is consistent with the project objective to obtain long target coverage in human. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Pizzonero M, et al. Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic. J Med Chem. 2014 Dec 11;57(23):10044-57.
溶解度数据
In Vitro: DMSO : 200 mg/mL (412.37 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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