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Rislenemdaz

    
98%

Rislenemdaz

源葉(MedMol)
S86578 一鍵復(fù)制產(chǎn)品信息
808732-98-1
C19H23FN4O2
358.4099232
貨號 規(guī)格 價(jià)格 上海 北京 武漢 南京 購買數(shù)量
S86578-1mg 98% ￥1500.00 貨期：2-3天 - - -
S86578-5mg 98% ￥4500.00 貨期：2-3天 - - -
S86578-10mg 98% ￥7500.00 貨期：2-3天 - - -
產(chǎn)品介紹 參考文獻(xiàn) 質(zhì)檢證書(COA) 摩爾濃度計(jì)算器 相關(guān)產(chǎn)品

產(chǎn)品介紹

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

產(chǎn)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
靶點(diǎn)： IC50: 3.6 nM (GluN2B) Ki: 8.1 nM (GluN2B);iGluR
體外研究： 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
體內(nèi)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
參考文獻(xiàn)： 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
保存條件： -20℃
配置溶液濃度參考：
1mg 5mg 10mg
1 mM 2.79 ml 13.951 ml 27.901 ml
5 mM 0.558 ml 2.79 ml 5.58 ml
10 mM 0.279 ml 1.395 ml 2.79 ml
50 mM 0.056 ml 0.279 ml 0.558 ml
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