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说明： Potent and selective negative allosteric modulator of mGlu1 receptors
化学名： 4-Fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide
纯度： ≥98% (HPLC)
生物活性 for FITM
FITM is a potent and selective negative allosteric modulator of mGlu1 receptors (IC50 = 5.1 nM). Displays >1300-fold selectivity for mGlu1 over other metabotropic glutamate receptors (IC50 values are 7 μM and >10 μM for mGlu5 and mGlu2 or mGlu8, respectively). Antagonizes methamphetamine-induced locomotion in mice.
化合物库 for FITM
FITM is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for FITM
| 分子量 | 371.43 |
| 公式 | C18H18FN5OS |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 932737-65-0 |
| PubChem ID | 16660135 |
| InChI Key | WIVGIKIKQHUFOD-UHFFFAOYSA-N |
| Smiles | CC(C)NC1=CC(=NC=N1)C1=CSC(=N1)N(C)C(=O)C1=CC=C(F)C=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 FITM
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 37.14 | 100 | |
| ethanol | 7.43 | 20 |
制备储备液 for FITM
以下数据基于产品分子量 371.43。 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 | 2.69 mL | 13.46 mL | 26.92 mL |
| 5 mM | 0.54 mL | 2.69 mL | 5.38 mL |
| 10 mM | 0.27 mL | 1.35 mL | 2.69 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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产品说明书 for FITM
参考文献 for FITM
参考文献是支持产品生物活性的出版物。
Satoh et al (2009) Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist. Bioorg.Med.Chem.Lett. 19 5464 PMID: 19674894
Wu et al (2014) Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator. Science. 344 58 PMID: 24603153
If you know of a relevant reference for FITM, please let us know.
关键词: FITM, FITM supplier, potent, selective, negative, allosteric, modulator, antagonist, mGlu1, group, I, metabotropic, glutamate, receptor, Glutamate, (Metabotropic), Group, Receptors, 6859, Tocris Bioscience
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Metabotropic Glutamate Receptors Scientific Review
Written by Francine Acher, this review discusses the pharmacology and therapeutic potential of mGlu receptors, and the compounds acting upon them; compounds available from Tocris are listed.
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