貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S86578-1mg	≥98%	￥1500.00 S86578-1mg ￥1500.00 2-3天	0 貨期：2-3天	-	-	-
S86578-5mg	≥98%	￥4500.00 S86578-5mg ￥4500.00 2-3天	0 貨期：2-3天	-	-	-
S86578-10mg	≥98%	￥7500.00 S86578-10mg ￥7500.00 2-3天	0 貨期：2-3天	-	-	-

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

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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