| 产品描述: | RO0711401 is a selective and orally active positive allosteric modulator of mGlu1 receptor with an EC50 of 56 nM |
| 靶点: |
mGluR1:56 nM (EC50);GluR |
| 体内研究: |
RO0711401 (10 mg/kg; s.c.; once) causes a long-lasting improvement in motor performance, which is maintained to the same extent at least for 6 days. Systemic injection of RO0711401 is shown to reduce the frequency of spike-and-wave discharges in a rat model of absence epilepsy, and to improve motor signs in autoimmune encephalomyelitis (EAE) mice. Animal Model: Spinocerebellar ataxia type 1 (SCA1) mice (30-week old) Dosage: 10 mg/kg Administration: Subcutaneous injection; once Result: Caused a prolonged improvement of motor performance on the rotarod and the paw-print tests. |
| 参考文献: |
1. Serena Notartomaso, et al. Pharmacological enhancement of mGlu1 metabotropic glutamate receptors causes a prolonged symptomatic benefit in a mouse model of spinocerebellar ataxia type 1. Mol Brain. 2013 Nov 19;6:48. 2. Eric Vieira, et al. Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1666-9. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.776 ml |
13.878 ml |
27.755 ml |
| 5 mM |
0.555 ml |
2.776 ml |
5.551 ml |
| 10 mM |
0.278 ml |
1.388 ml |
2.776 ml |
| 50 mM |
0.056 ml |
0.278 ml |
0.555 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |