1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. iGluR
  3. GYKI 52466 dihydrochloride

GYKI 52466 dihydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 dihydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 dihydrochloride can be used in Parkinson's disease research.

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GYKI 52466 dihydrochloride

GYKI 52466 dihydrochloride Chemische Struktur

CAS. Nr. : 2319722-40-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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Beschreibung

GYKI 52466 dihydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 dihydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 dihydrochloride can be used in Parkinson's disease research[1][2].

IC50 & Target[1]

Kainate Receptor

11 μM (IC50)

In Vitro

GYKI 52466 (0.3-100 μM) inhibits inward currents activated by AMPA and Kainate receptor in cultured rat hippocampal neurons[1].

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

In Vivo

GYKI 52466 (intraperitoneal injection; 1.76-13.2 mg/kg; once) treatment provides potent anticonvulsant protection against sound-induced seizures in DBA/2 mice[2].

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

Animal Model: Male and female DBA/2 mice tested for sound-induced seizure responses[2]
Dosage: 1.76-13.2 mg/kg
Administration: Intraperitoneal injection; 1.76-13.2 mg/kg; once
Result: Observed Maximal anticonvulsant protection after the i.p. treatment (5-15 min ).
Molekulargewicht

366.24

Formel

C17H17Cl2N3O2

CAS. Nr.
Appearance

Solid

Color

Yellow to orange

SMILES

NC1=CC=C(C2=NN=C(C)CC3=CC4=C(OCO4)C=C32)C=C1.[H]Cl.[H]Cl

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

4°C, sealed storage, away from moisture and light

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

Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 10 mg/mL (27.30 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7304 mL 13.6523 mL 27.3045 mL
5 mM 0.5461 mL 2.7304 mL 5.4609 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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molaritätsrechner

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Reinheit & Dokumentation
Verweise

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 and light). 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
DMSO 1 mM 2.7305 mL 13.6523 mL 27.3045 mL 68.2613 mL
5 mM 0.5461 mL 2.7305 mL 5.4609 mL 13.6523 mL
10 mM 0.2730 mL 1.3652 mL 2.7305 mL 6.8261 mL
15 mM 0.1820 mL 0.9102 mL 1.8203 mL 4.5508 mL
20 mM 0.1365 mL 0.6826 mL 1.3652 mL 3.4131 mL
25 mM 0.1092 mL 0.5461 mL 1.0922 mL 2.7305 mL
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    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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Produktname:
GYKI 52466 dihydrochloride
Art. -Nr.:
HY-103234A
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