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Submit ReviewGLPG 0974 is a potent FFA2 antagonist (IC50 = 9 nM). Exhibits selectivity for FFA2 over FFA3. Inhibits acetate-induced human neutrophil migration in plasma or buffer. Also inhibits FFA2-induced expression of CD11b activation-specific epitope (AE) in human whole blood. Orally bioavailable.
GLPG 0974 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 485 |
公式 | C25H25ClN2O4S |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1391076-61-1 |
PubChem ID | 57520598 |
InChI Key | MPMKMQHJHDHPBE-RUZDIDTESA-N |
Smiles | O=C(N1[C@](C(N(CC2=CC(Cl)=CC=C2)CCCC(O)=O)=O)(C)CC1)C3=CSC4=C3C=CC=C4 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 48.5 | 100 | |
ethanol | 48.5 | 100 |
以下数据基于产品分子量 485。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.06 mL | 10.31 mL | 20.62 mL |
5 mM | 0.41 mL | 2.06 mL | 4.12 mL |
10 mM | 0.21 mL | 1.03 mL | 2.06 mL |
50 mM | 0.04 mL | 0.21 mL | 0.41 mL |
参考文献是支持产品生物活性的出版物。
Pizzonero et al (2014) Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic. J.Med.Chem. 57 10044 PMID: 25380412
If you know of a relevant reference for GLPG 0974, please let us know.
关键词: GLPG 0974, GLPG 0974 supplier, GLPG0974, free, fatty, acid, receptors, FFA2, antagonists, antagonism, potent, Free, Fatty, Acid, Receptors, 5621, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 GLPG 0974 的部分引用包括:
Marco et al (2020) Acetate coordinates neutrophil and ILC3 responses against C. difficile through FFAR2. J Exp Med 217 PMID: 31876919
Tsung-Hsien et al (2020) Leuconostoc mesenteroides fermentation produces butyric acid and mediates Ffar2 to regulate blood glucose and insulin in type 1 diabetic mice. Sci Rep 10 7928 PMID: 32404878
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