产品说明书
Riluzole
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同义名 : | PK 26124;RP-54274;Riluzole, Rilutek, PK 26124, PK26124, PK-26124, RP 54274, RP54274 |
| CAS号 : | 1744-22-5 | |
| 货号 : | A221527 | |
| 分子式 : | C8H5F3N2OS | |
| 纯度 : | 97% | |
| 分子量 : | 234.2 | |
| MDL号 : | MFCD00210213 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(448.33 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 1 mg/mL(4.27 mM)，配合低频超声，并调节pH至3 |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+40% PEG300+water 10 mg/mL clear PO 0.5% CMC-Na 56 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | Riluzole, classified as an anticonvulsant, functions as a use-dependent sodium channel blocker and also exhibits the ability to inhibit GABA uptake, with an IC50 of 43 μM. It shows slight inhibition of peak autaptic IPSCs at a concentration of 20 μM, but it reliably prolongs IPSCs at this level. More notably, Riluzole significantly enhances responses to 2 μM GABA in a concentration-dependent and readily reversible manner. At a higher concentration of 300 μM, it leads to apparent desensitization of GABA currents during prolonged exposure to 2 μM GABA. The effective concentration (EC50) for Riluzole's potentiation of GABA responses is approximately 60 μM[1]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT03359538 | Amyotrophic Lateral Sclerosis | Phase 2 | Recruiting | September 19, 2019 | Italy ... 展开 >> Centro Sla, Irccs A.O.U. S.Martino Ist, Genova Not yet recruiting Genova, Italy Contact: Claudia Caponnetto, MD Centro Clinico Nemo, Fondazione Serena Onlus, Milano Not yet recruiting Milano, Italy Contact: Christian Lunetta, MD Centro Sla, Irccs Fondazione Salvatore Maugeri, Milano Not yet recruiting Milano, Italy Contact: Kalliopi Marinou, MD Centro Sla, Irccs Istituto Carlo Besta, Milano Not yet recruiting Milano, Italy Contact: Eleonora Dalla Bella, MD Centro Sla, Ospedale Civile S. Agostino Estense, A.O.U. Modena Recruiting Modena, Italy, 41126 Contact: Jessica Mandrioli, MD +390593961722 Centro Sla, A.O.U. Maggiore Della Carita', Novara Not yet recruiting Novara, Italy Contact: Letizia Mazzini, MD Centro Sla, Universita' Di Padova Not yet recruiting Padova, Italy Contact: Gianni Sorarù, MD Centro Sla, Universita' Di Torino Not yet recruiting Torino, Italy Contact: Adriano Chiò, Prof. 收起 << |
| NCT01378676 | Amyotrophic Lateral Sclerosis | Phase 2 | Completed | - | United States, California ... 展开 >> California Pacific Medical Center San Francisco, California, United States, 94115 United States, Florida Mayo Florida Jacksonville, Florida, United States, 32224 United States, Kansas University of Kansas Kansas City, Kansas, United States, 06053 United States, Maryland Johns Hopkins Hospital Baltimore, Maryland, United States, 21287 United States, New York Columbia University Medical Center New York, New York, United States, 10032 SUNY Upstate Medical Center Syracuse, New York, United States, 13210 United States, North Carolina Carolinas Neuromuscular ALS-MND Center Charlotte, North Carolina, United States, 28207 United States, Pennsylvania Penn State Hershey Medical Center Hershey, Pennsylvania, United States, 17033 Drexel University College of Medicine Philadelphia, Pennsylvania, United States, 19107 收起 << |
| NCT00560287 | Amyotrophic Lateral Sclerosis ... 展开 >> Chronic Respiratory Failure 收起 << | Phase 4 | Unknown | August 2010 | Italy ... 展开 >> Fondazione S.Maugeri Recruiting Pavia, Italy, 27100 Contact: Stefano Nava, md o3825921 snava@fsm.it Contact: Stefano Nava, md 03825921 snava@fsm.it Respiratory Unit FSM Not yet recruiting Pavia, Italy, 27100 Contact: Stefano Nava, md 0382 592 ext 806 snava@fsm.it Contact: Francesco Fanfulla, MD 0382 592 ext 815 ffanfulla@fsm.it Principal Investigator: Stefano Nava, MD 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
4.27mL 0.85mL 0.43mL |
21.35mL 4.27mL 2.13mL |
42.70mL 8.54mL 4.27mL |
| 参考文献 |
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