| 货号 | 规格 | 价格 | 上海 | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|
| S86578-1mg | 98% | ￥1500.00 | 货期：2-3天 | - | - | - |
|
| S86578-5mg | 98% | ￥4500.00 | 货期：2-3天 | - | - | - |
|
| S86578-10mg | 98% | ￥7500.00 | 货期：2-3天 | - | - | - |
|
Rislenemdaz (CERC-301) is an orally bioavailable and selective N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) antagonist with Ki and IC50 of 8.1 nM and 3.6 nM, respectively
| 产品描述： | Rislenemdaz (CERC-301) is an orally bioavailable and selective N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) antagonist with Ki and IC50 of 8.1 nM and 3.6 nM, respectively | ||||||||||||||||||||
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| 靶点： | IC50: 3.6 nM (GluN2B) Ki: 8.1 nM (GluN2B);iGluR | ||||||||||||||||||||
| 体外研究： | Rislenemdaz (CERC-301) inhibits calcium influx into agonist-stimulating NMDA-GluN1a/GluN2B L(tk-) cells with an IC50 of 3.6 nM. Rislenemdaz exhibits at least 1000× selectivity for the GluN2B receptor versus all targets tested, including the hERG potassium channel. Rislenemdaz also exhibits minimal activity against sigma-type receptors at 10 uM | ||||||||||||||||||||
| 体内研究： | Rislenemdaz (CERC-301) (1, 3, 10, and 30 mg/kg) significantly decreases immobility frequency (P<0.001) and significantly increases swimming behavior (P<0.01 for 1, 3, and 30 mg/kg; P<0.05 for 10 mg/kg) compare to the vehicle control. Rislenemdaz plasma levels are approximately 15, 120, 390, 1420, 4700, and 14,110 nM (0.015, 0.120, 0.390, 1.42, 4.7, and 14.11 uM) at the time of sampling, corresponding to approximately 5, 29, 56, 83, 94, and 98% RO, respectively, in rats. The ED50 for increaing in frequency of swimming and decreasing in immobility are ~0.3 and 0.7 mg/kg, respectively, corresponding to RO of ~30 and 50%. Rislenemdaz (1, 3, 10, and 30 mg/kg) significantly increases total distance traveling (P<0.01 for 1 mg/kg; P<0.001 for 3, 10, and 30 mg/kg) compare to vehicle control over the 60 min test | ||||||||||||||||||||
| 参考文献： | 1. Rachel Garner, et al. Preclinical pharmacology and pharmacokinetics of CERC‐301, a GluN2B‐selective N‐methyl‐D‐aspartate receptor antagonist. Pharmacol Res Perspect. 2015 Dec; 3(6): e00198. | ||||||||||||||||||||
| 溶解性： | soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 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。 |
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