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
- 화학식: C22H26N2O2S2
- 분자량:414.58
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
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
-
분자량 414.58
-
화학식 C22H26N2O2S2
-
SMILES
OC1=NOC2=C1C(CCC2)N(C)CC/C=C(C3=C(C=CS3)C)\C4=C(C=CS4)C
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)