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Cat. No.: HY-118931

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EF-1502

EF-1502 is a potent and selective GABA transporter inhibitor with GAT1 and BGT1 inhibitory activity. EF-1502 produces a synergistic anti-epileptic effect when used in combination with Tiagabine (HY-B0696), a compound used to suppress epileptic seizures. The dosing combination of EF-1502 exhibited reduced anti-epileptic efficacy and dyskinesia when used with THIP (HY-10232). The mechanism of EF-1502 differs significantly from Tiagabine, suggesting a unique role in the inhibitory strategy.

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CAS No.: 684645-54-3
Formule: C₂₂H₂₆N₂O₂S₂
Masse moléculaire:414.58

Stockage:

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

Data Sheet (271 KB)

EF-1502 Chemical Structure

CAS No.: 684645-54-3

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Use of MCE Products

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

Activité biologique
- Description
- Cellular Effect
Chemical Information
Pureté et documentation
Références
Calculators
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Classifications
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Activité biologique

Description

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	>300 μM Compound: 5, EF1502	Inhibition of [3H]GABA uptake at mouse GAT3 expressed in HEK293 cells after 3 mins by scintillation counting analysis Inhibition of [3H]GABA uptake at mouse GAT3 expressed in HEK293 cells after 3 mins by scintillation counting analysis	[PMID: 23398473]
HEK293	IC₅₀	>300 μM Compound: 5, EF1502	Inhibition of [3H]GABA uptake at mouse GAT4 expressed in HEK293 cells after 3 mins by scintillation counting analysis Inhibition of [3H]GABA uptake at mouse GAT4 expressed in HEK293 cells after 3 mins by scintillation counting analysis	[PMID: 23398473]
HEK293	IC₅₀	>300 μM Compound: 9, EF1502	Inhibition of mouse GAT3-mediated [3H]GABA uptake expressed in human HEK cells Inhibition of mouse GAT3-mediated [3H]GABA uptake expressed in human HEK cells	[PMID: 21353350]
HEK293	IC₅₀	>300 μM Compound: 9, EF1502	Inhibition of mouse GAT4-mediated [3H]GABA uptake expressed in human HEK cells Inhibition of mouse GAT4-mediated [3H]GABA uptake expressed in human HEK cells	[PMID: 21353350]
HEK293	IC₅₀	22 μM Compound: 9, EF1502	Inhibition of mouse GAT2-mediated [3H]GABA uptake expressed in human HEK cells Inhibition of mouse GAT2-mediated [3H]GABA uptake expressed in human HEK cells	[PMID: 21353350]
HEK293	IC₅₀	26 μM Compound: 5, EF1502	Inhibition of [3H]GABA uptake at mouse GAT2 expressed in HEK293 cells after 3 mins by scintillation counting analysis Inhibition of [3H]GABA uptake at mouse GAT2 expressed in HEK293 cells after 3 mins by scintillation counting analysis	[PMID: 23398473]
HEK293	IC₅₀	4 μM Compound: 9, EF1502	Inhibition of mouse GAT1-mediated [3H]GABA uptake expressed in human HEK cells Inhibition of mouse GAT1-mediated [3H]GABA uptake expressed in human HEK cells	[PMID: 21353350]
HEK293	IC₅₀	7 μM Compound: 5, EF1502	Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 3 mins by scintillation counting analysis Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 3 mins by scintillation counting analysis	[PMID: 23398473]

Chemical Information

CAS No. 684645-54-3
Masse moléculaire 414.58
Formule C₂₂H₂₆N₂O₂S₂
SMILES

OC1=NOC2=C1C(CCC2)N(C)CC/C=C(C3=C(C=CS3)C)\C4=C(C=CS4)C
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 (271 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]. Selective GABA transporter inhibitors tiagabine and EF1502 exhibit mechanistic differences in their ability to modulate the ataxia and anticonvulsant action of the extrasynaptic GABA(A) receptor agonist gaboxadol [Content Brief]

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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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