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  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.

For research use only. We do not sell to patients.

GYKI 52466 dihydrochloride Chemical Structure

GYKI 52466 dihydrochloride Chemical Structure

CAS No. : 2319722-40-0

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Based on 1 publication(s) in Google Scholar

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Description

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 ).
Molecular Weight

366.24

Formula

C17H17Cl2N3O2

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Solvent & Solubility
In Vitro: 

DMSO : 2.78 mg/mL (7.59 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.

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
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GYKI 52466 dihydrochloride Related Classifications

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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Product Name:
GYKI 52466 dihydrochloride
Cat. No.:
HY-103234A
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