2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. NMDA receptor antagonist 4

NMDA receptor antagonist 4 

目录号: HY-146588 纯度: 99.64%
COA 产品使用指南

摩尔计算器

NMDA receptor antagonist 4 (IIc) 是一个非竞争性、电压依赖的、具有口服活性的 NMDAR 阻断剂，其 IC50 值为1.93 µM。NMDA receptor antagonist 4 可透过血脑屏障，能被用于研究阿兹海默症 (Alzheimer's disease)。

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NMDA receptor antagonist 4 Chemical Structure

NMDA receptor antagonist 4 Chemical Structure

CAS No. : 1607589-56-9

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1 mg ￥3580
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NMDA receptor antagonist 4 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NMDA receptor antagonist 4 (IIc) is a uncompetitive, voltage-dependent, orally active NMDAR blocker, with an IC50 of 1.93 µM. NMDA receptor antagonist 4 shows a positive predicted blood-brain-barrier (BBB) permeability, and can be studied in Alzheimer's disease[1].

IC50 & Target

IC50: 1.93 µM (NMDAR)[1]
体外研究
(In Vitro)

NMDA receptor antagonist 4 (IIc) shows competitive interaction with endogenous blocker Mg2+, and shows dependence on membrane potential in the NMDAR channel[1].
NMDA receptor antagonist 4 shows high metabolic stability in human and mice liver microsomes, and shows hERG safety, without obvious cytotoxicity[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

NMDA receptor antagonist 4 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: Neuro2A cells
Concentration: 1, 10, and 100 µM
Incubation Time: 24 h
Result: Did not show cytotoxic at the highest concentration tested (100 µM).
体内研究
(In Vivo)

NMDA receptor antagonist 4 (IIc) (0-10 µM) rescues the motor deficits, and protects against Aβ toxicity-related neuronal dysfunction[1].
NMDA receptor antagonist 4 (5 mg/kg/day; p.o.; 4 weeks) improves cell survival and synaptic function in AD through increasing the activity of cell-survival signaling pathways (Fyn-GluN2B-CREB signaling) and preventing internalization of synaptic NMDARs[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C. elegans (N2 wild-type, CL2006, CL2122, CL2355)[1]
Dosage: 0, 0.1, 0.5, 1.5, and 10 µM
Administration:
Result: Reduced defective locomotion in CL2006 nematodes. Significantly reversed the chemotaxis behavior of CL2355 nematodes disrupted by Aβ expression.
Animal Model: Six months old female 5XFAD mice[1]
Dosage: 5 mg/kg/day
Administration: Oral administration, 4 weeks
Result: Enhanced working memory function. Rescued the expression of GluN2A and postsynaptic density protein (PSD) 95. Increased Fyn phosphorylated levels and correspondingly elevated GluN2B phosphorylation at Tyr1472. Significantly increased p-CREB protein levels in the nucleus. Reverted calbindin D-28K protein levels.
分子量

231.31

Formula

C15H18FN
CAS 号
性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 125 mg/mL (540.40 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.3232 mL 21.6160 mL 43.2320 mL
5 mM 0.8646 mL 4.3232 mL 8.6464 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

NMDA receptor antagonist 4 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.3232 mL 21.6160 mL 43.2320 mL 108.0801 mL
5 mM 0.8646 mL 4.3232 mL 8.6464 mL 21.6160 mL
10 mM 0.4323 mL 2.1616 mL 4.3232 mL 10.8080 mL
15 mM 0.2882 mL 1.4411 mL 2.8821 mL 7.2053 mL
20 mM 0.2162 mL 1.0808 mL 2.1616 mL 5.4040 mL
25 mM 0.1729 mL 0.8646 mL 1.7293 mL 4.3232 mL
30 mM 0.1441 mL 0.7205 mL 1.4411 mL 3.6027 mL
40 mM 0.1081 mL 0.5404 mL 1.0808 mL 2.7020 mL
50 mM 0.0865 mL 0.4323 mL 0.8646 mL 2.1616 mL
60 mM 0.0721 mL 0.3603 mL 0.7205 mL 1.8013 mL
80 mM 0.0540 mL 0.2702 mL 0.5404 mL 1.3510 mL
100 mM 0.0432 mL 0.2162 mL 0.4323 mL 1.0808 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NMDA receptor antagonist 41607589-56-9NMDA receptor antagonist4NMDA receptor antagonist-4iGluRIonotropic glutamate receptorsC. elegans5XFADMemantine analogsInhibitorinhibitorinhibit

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