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  3. GYKI 53655 hydrochloride

GYKI 53655 hydrochloride  (Synonyms: LY300168 hydrochloride)

目录号: HY-103228 纯度: 98.15%
COA 产品使用指南

GYKI 53655 (LY300168) hydrochloride 是 α-氨基-3-羟基-5-甲基异恶唑-4-丙酸 (AMPA) 的拮抗剂。

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GYKI 53655 hydrochloride Chemical Structure

GYKI 53655 hydrochloride Chemical Structure

CAS No. : 143692-48-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1320
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1 mg ¥545
In-stock
5 mg ¥1200
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10 mg ¥1700
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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

GYKI 53655 (LY300168) hydrochloride is an α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) antagonist.

IC50 & Target

AMPA[1]

体外研究
(In Vitro)

GYKI 53655 (LY300168) hydrochloride inhibits α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) (10 μM)-induced responses with IC50 value of 5.9±0.1 μM. GYKI 53655 hydrochloride inhibits AMPA (10 μM) responses in recombinant G1uR4 expressing HEK293 cells with IC50 value of 4.6±0.4 μM. Using 3 μM cyclothiazide the inhibition produced by GYKI 53655 hydrochloride is 79±2% (n=4 cells). GYKI 53655 hydrochloride produces only small inhibitions of kainate-induced currents at 30 μM and inhibits kainate-induced currents at a concentration of 100 μM by 12±2 (n=4) and 18±4 (n=4), respectively. GYKI 53655 hydrochloride inhibits AMPA receptor-mediated responses in cerebella Purkinje neurons with an IC50 value of 1.5±0.1 μM[1].

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

体内研究
(In Vivo)

GYKI 53655 hydrochloride (4 mg/kg) is found to have a short-lasting depressant effect on neuronal responses to iontophoretic α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA), with a half-recovery time of approximately 7 min. GYKI 53655 hydrochloride (4 and 8 mg/kg) substantially depresses or completely abolishes AMPA responses. Results demonstrate the dose-dependence of GYKI 53655 hydrochloride (2 to 8 mg/kg) in depressing responses to AMPA. At the highest doses tested, GYKI 53655 hydrochloride reduces AMPA responses to a comparable degree[2]. Tonic fit and death are completely prevented by GYKI 53655 hydrochloride at dose over 5.0 mg/kg. The ED50 value of GYKI 53655 hydrochloride is 2.2 mg/kg i.p. The maximal effects of GYKI 53655 hydrochloride lasts 3 h then the exit inhibition effect of GYKI 53655 hydrochloride falls to 20% 1 h later[3].

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

分子量

388.85

Formula

C19H21ClN4O3

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 160 mg/mL (411.47 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : 8 mg/mL (20.57 mM; 超声加热助溶)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5717 mL 12.8584 mL 25.7169 mL
5 mM 0.5143 mL 2.5717 mL 5.1434 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 (sealed storage, away from moisture)。-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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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
参考文献
Cell Assay
[1]

Whole-cell voltage clamp recordings are made from single cells with use of the tight seal whole cell configuration of the patch-clamp technique. Experiments are performed at room temperature (20 to 22°C) and recorded on an amplifier. GYKI 53655 hydrochloride application is via a series of perfusion lines to a multi-barrelled applicator and exchange of solutions under the present recording conditions is approximately 100 msec. For the acutely isolated cerebella Purkinje neurons, GYKI 53655 hydrochloride application is by bath perfusion and occurs within approximately 15 sec. Curve fitting to data points is based upon the equationy=100(Dn/(Dn+IC50n)), where the slope of the line n is fixed to a value of 1 and D is the antagonist concentration. Statistical significance is determined by one-way ANOVA followed by Student- Newman-Keulstest[1].

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

Animal Administration
[2]

Experiments are performed on 27 male Wistar rats (260 to 350 g). Briefly, rats are anaesthetized with halothane in O2 and tracheal, carotid and jugular cannulae are inserted. The lumbo-thoracic spinal cord is exposed and cut at T9-T11 and the animal is prepared for extracellular recordings of single dorsal horn neurone action potentials. Anaesthesia after surgery is maintained with α-chloralose. Jugular cannulae are inserted. GYKI 53655 hydrochloride is administered intravenously. The effect of GYKI 53655 hydrochloride is expressed quantitatively as percentages of control excitatory amino acids (EAA) responses, where control is taken as the mean of the last 3 pre-drug counts; mean values±s.e.mean are indicated. No corrections for spontaneous activity are made[2].

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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
H2O / DMSO 1 mM 2.5717 mL 12.8584 mL 25.7169 mL 64.2921 mL
5 mM 0.5143 mL 2.5717 mL 5.1434 mL 12.8584 mL
10 mM 0.2572 mL 1.2858 mL 2.5717 mL 6.4292 mL
15 mM 0.1714 mL 0.8572 mL 1.7145 mL 4.2861 mL
20 mM 0.1286 mL 0.6429 mL 1.2858 mL 3.2146 mL
DMSO 25 mM 0.1029 mL 0.5143 mL 1.0287 mL 2.5717 mL
30 mM 0.0857 mL 0.4286 mL 0.8572 mL 2.1431 mL
40 mM 0.0643 mL 0.3215 mL 0.6429 mL 1.6073 mL
50 mM 0.0514 mL 0.2572 mL 0.5143 mL 1.2858 mL
60 mM 0.0429 mL 0.2143 mL 0.4286 mL 1.0715 mL
80 mM 0.0321 mL 0.1607 mL 0.3215 mL 0.8037 mL
100 mM 0.0257 mL 0.1286 mL 0.2572 mL 0.6429 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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:
GYKI 53655 hydrochloride
目录号:
HY-103228
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