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製品番号: 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 番号: 684645-54-3
分子式: C₂₂H₂₆N₂O₂S₂
分子量:414.58

保管条件:

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

Data Sheet (271 KB)

EF-1502 構造式

CAS 番号: 684645-54-3

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性

製品説明

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]

化学情報

CAS 番号 684645-54-3
分子量 414.58
分子式 C₂₂H₂₆N₂O₂S₂
SMILES

OC1=NOC2=C1C(CCC2)N(C)CC/C=C(C3=C(C=CS3)C)\C4=C(C=CS4)C
輸送条件

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

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (271 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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?

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100 mg

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