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说明： Potent and selective tryptophan 2,3-dioxygenase (TDO) inhibitor
化学名： 6-Fluoro-3-[(1E)-2-(3-pyridinyl)ethenyl]-1H-indole
纯度： ≥98% (HPLC)
生物活性 for 680C91
680C91 is a potent and selective inhibitor of tryptophan 2,3-dioxygenase (TDO) (Ki = 51 nM). Exhibits no activity against indoleamine 2,3-dioxygenase, monoamine oxidase A and B, 5-HT uptake or 5-HT1A, 1D, 2A and 2C receptors. Produces large increases in brain tryptophan and serotonin in vitro and in vivo in the rat.
技术数据 for 680C91
| 分子量 | 238.26 |
| 公式 | C15H11FN2 |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 163239-22-3 |
| PubChem ID | 10014426 |
| InChI Key | YBSDQTBCNYWBMX-ONEGZZNKSA-N |
| Smiles | FC1=CC=C2C(NC=C2/C=C/C3=CN=CC=C3)=C1 |
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.
溶解性数据 for 680C91
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 23.83 | 100 | |
| ethanol | 11.91 | 50 |
制备储备液 for 680C91
以下数据基于产品分子量 238.26。 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 | 4.2 mL | 20.99 mL | 41.97 mL |
| 5 mM | 0.84 mL | 4.2 mL | 8.39 mL |
| 10 mM | 0.42 mL | 2.1 mL | 4.2 mL |
| 50 mM | 0.08 mL | 0.42 mL | 0.84 mL |
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产品说明书 for 680C91
参考文献 for 680C91
参考文献是支持产品生物活性的出版物。
Salter et al (1995) The effects of a novel and selective inhibitor of tryptophan 2,3-dioxygenase on tryptophan and serotonin metabolism in the rat. Biochem.Pharmacol. 17 1435 PMID: 7539265
Salter et al (1995) The effects of an inhibitor of tryptophan 2,3-dioxygenase and a combined inhibitor of tryptophan 2,3-dioxygenase and 5-HT reuptake in the rat. Neuropharmacology 34 217 PMID: 7617147
Opitz et al (2011) An endogenous tumour-promoting ligand of the human aryl hydrocarbon receptor. Nature 478 197 PMID: 21976023
If you know of a relevant reference for 680C91, please let us know.
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关键词: 680C91, 680C91 supplier, tryptophan, 2,3-dioxygenase, inhibits, TDO, inhibitors, catabolism, immune, checkpoints, Tryptophan, 2,3, dioxygenase, Immune, Checkpoints, 4392, Tocris Bioscience
5 篇 680C91 的引用文献
引用文献是使用了 Tocris 产品的出版物。 680C91 的部分引用包括：
Alan J et al (2021) Inhibition of tryptophan 2,3-dioxygenase impairs DNA damage tolerance and repair in glioma cells. NAR Cancer 3 zcab014 PMID: 33870196
Bostian et al (2016) Kynurenine Signaling Increases DNA Polymerase Kappa Expression and Promotes Genomic Instability in Glioblastoma Cells. Chem Res Toxicol 29 101 PMID: 26651356
D'Amato et al (2015) A TDO2-AhR Signaling Axis Facilitates Anoikis Resistance and Metastasis in Triple-Negative Breast Cancer. Cancer Res 75 4651 PMID: 26363006
Breda et al (2016) Tryptophan-2,3-dioxygenase (TDO) inhibition ameliorates neurodegeneration by modulation of kynurenine pathway metabolites. Proc.Natl.Acad.Sci.U.S.A. 113 5435 PMID: 27114543
Howard L et al (2019) Control of tumor-associated macrophages and T cells in glioblastoma via AHR and CD39. Nat Neurosci 22 729-740 PMID: 30962630
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