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Cat. No.: HY-19259

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GP3269

GP3269 is a selective and orally active human adenosine kinase (AK) inhibitor with an IC₅₀ of 11 nM against human adenosine kinase. GP3269 increases adenosine levels at epileptic foci, activates A1 receptors on excitatory neurons, and exhibits anticonvulsant activity in rats. GP3269 does not induce hemodynamic effects including changes in blood pressure or heart rate in rats. GP3269 can be used for epilepsy-related research.

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CAS No.: 186393-42-0
Formule: C₂₃H₂₁FN₄O₃
Masse moléculaire:420.44

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

GP3269 Chemical Structure

CAS No.: 186393-42-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Cellular Effect

Cell Line	Type	Value	Description	References
IMR-32	IC₅₀	134 nM Compound: 4	Inhibition of adenosine phosphorylation in confluent IMR-32 (human neuroblastoma) cells. Inhibition of adenosine phosphorylation in confluent IMR-32 (human neuroblastoma) cells.	[PMID: 11405650]

In Vitro

GP3269 (20 minutes at 37 °C) potently inhibits purified pig heart adenosine kinase with an IC₅₀ of 11 nM^[1].

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

In Vivo

GP3269 (p.o.) suppresses seizures in the MES rat model with an ED₅₀ of 5.1 mg/kg^[1].
GP3269 has an oral bioavailability of 60% and a plasma half-life of 4.2 h in dogs^[1].

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

Chemical Information

CAS No. 186393-42-0
Masse moléculaire 420.44
Formule C₂₃H₂₁FN₄O₃
SMILES

O[C@H]([C@@H]([C@H](O1)C)O)[C@]1([H])N2C3=NC=NC(NC4=CC=C(C=C4)F)=C3C(C5=CC=CC=C5)=C2
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Erion M D, et al. Design, synthesis and anticonvulsant activity of the potent adenosine kinase inhibitor GP3269. Nucleosides, Nucleotides & Nucleic Acids, 1997, 16(7-9): 1013-1021.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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