1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. iGluR
  3. MDL 105519

MDL 105519是有效和选择性的甘氨酸与 NMDA 受体结合的拮抗剂。

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MDL 105519 Chemical Structure

MDL 105519 Chemical Structure

CAS No. : 161230-88-2

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10 mM * 1 mL in DMSO ¥1100
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5 mg ¥1000
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10 mg ¥1700
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25 mg ¥3600
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Other Forms of MDL 105519:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

MDL 105519 is a potent and selective antagonist of glycine binding to the NMDA receptor.

体外研究
(In Vitro)

MDL 105519 is a potent and selective ligand for the glycine recognition site that completely inhibit the binding of [3H]glycine to rat brain membranes with a Ki value of 10.9 nM. MDL 105519 is approximately 10,000-fold selective for the glycine recognition site relative to the other receptor types investigated. MDL 105519 inhibits NMDA-dependent responses, such as elevations of [3H]TCP binding in brain membranes, cyclic GMP accumulation in brain slices, and alterations in cytosolic Ca2+ and Na+-Ca2+ currents in cultured neurons. Inhibition is non-competitive with respect to NMDA and could be nullified with D-serine[1].

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

体内研究
(In Vivo)

MDL 105519 is an NMDA receptor antagonist in vivo. Intravenously administration of MDL 105519 prevents harmaline-stimulated increases in cerebellar cyclic GMP content, providing biochemical evidence of NMDA receptor antagonism in vivo. This antagonism is associated with anticonvulsant activity in genetically based, chemically induced, and electrically mediated seizure models. Anxiolytic activity is observed in the rat separation-induced vocalization model, but muscle-relaxant activity is apparent at lower doses. Higher doses impair rotorod performance, but are without effect on mesolimbic dopamine turnover or prepulse inhibition of the startle reflex[1].

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

分子量

376.19

Formula

C18H11Cl2NO4

CAS 号
性状

固体

颜色

Off-white to 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 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 17 mg/mL (45.19 mM; 超声加热助溶; 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 2.6582 mL 13.2912 mL 26.5823 mL
5 mM 0.5316 mL 2.6582 mL 5.3165 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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

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

纯度: 99.67%

参考文献
Animal Administration
[1]

Adult, male, CD rats are administered MK-801 (n=4, 2 mg/kg, i.p.) or MDL 105519 (n=4, 2 mg/kg, i.p.) and extracellular dopamine concentrations are measured using in vivo microdialysis[1].

Mice: Mice adult male CD-1 are injected with various doses of MDL 105519 (8, 16, 32, 64, 128 mg/kg) intraperitoneally and 30 min later are administered harmaline 50 mg/kg. Sixty minutes after the first injection, the mice are killed and cerebellar cGMP content is measured by radioimmunoassay[1].

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

参考文献

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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6582 mL 13.2912 mL 26.5823 mL 66.4558 mL
5 mM 0.5316 mL 2.6582 mL 5.3165 mL 13.2912 mL
10 mM 0.2658 mL 1.3291 mL 2.6582 mL 6.6456 mL
15 mM 0.1772 mL 0.8861 mL 1.7722 mL 4.4304 mL
20 mM 0.1329 mL 0.6646 mL 1.3291 mL 3.3228 mL
25 mM 0.1063 mL 0.5316 mL 1.0633 mL 2.6582 mL
30 mM 0.0886 mL 0.4430 mL 0.8861 mL 2.2152 mL
40 mM 0.0665 mL 0.3323 mL 0.6646 mL 1.6614 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.

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产品名称:
MDL 105519
目录号:
HY-15085
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