2. Membrane Transporter/Ion Channel Neuronal Signaling
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  4. GYKI 53655 hydrochloride

GYKI 53655 (hydrochloride)  (Synonyms: LY300168 (hydrochloride))

製品番号: HY-103228 純度: 98.37%
COA 取扱説明書 Technical Support

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

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GYKI 53655 hydrochloride

GYKI 53655 (hydrochloride) 構造式

CAS 番号 : 143692-48-2

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 在庫あり
Solution
10 mM * 1 mL in DMSO USD 132 在庫あり
Solid
5 mg $120 在庫あり
10 mg $170 在庫あり
25 mg $374 在庫あり
50 mg $690 在庫あり
100 mg $1200 在庫あり
200 mg   お問い合わせ  
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GYKI 53655 (hydrochloride) 関連抗体

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AMPA Receptor NMDA Receptor Kainate Receptor

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製品説明

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

IC50 & Target

AMPA[1]
体外実験

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].

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

GYKI 53655 (hydrochloride) 関連抗体
体内実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

388.85

分子式

C19H21ClN4O3
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N1N=C(C2=CC=C(N)C=C2)C3=CC(OCO4)=C4C=C3CC1C)NC.[H]Cl
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

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

DMSO : ≥ 160 mg/mL (411.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 8 mg/mL (20.57 mM; Need ultrasonic and warming)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
10 mM 0.2572 mL 1.2858 mL 2.5717 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

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体積 （開始）

V1

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In Vivo Dissolution Calculator
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純度とドキュメンテーション

純度: 98.37%

COA (252 KB) HNMR (141 KB) LCMS (95 KB)

取扱説明書 (2659 KB)
参考文献
細胞実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
動物実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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GYKI 53655 hydrochloride Related Classifications

  • Molarity Calculator

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The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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Keywords:

GYKI 53655143692-48-2LY300168GYKI53655GYKI-53655LY 300168LY-300168iGluRIonotropic glutamate receptorsInhibitorinhibitorinhibit

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