PF-05020182
PF-05020182 is an orally active opener for Kv7 channel, that activates human Kv7.2/7.3, Kv7.4 and Kv7.3/7.5 with EC50 of 334, 625 and 588 nM, respectively. PF-05020182 exhibits anticonvulsant activity in rats corneal electric shock-induced tonic seizure (MES) models. PF-05020182 is blood-brain barrier (BBB) penetrable.
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- CAS. Nr.: 1354712-92-7
- Formel: C18H30N4O4
- Molecular Weight:366.46
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
1327 nM
Compound: 2, PF-05020182
|
Activation of rat Kv7.3/7.5 expressed in CHOK1 cells
Activation of rat Kv7.3/7.5 expressed in CHOK1 cells
|
[PMID: 25987375] |
| CHO-K1 | EC50 |
294 nM
Compound: 2, PF-05020182
|
Activation of rat Kv7.2/7.3 expressed in CHOK1 cells
Activation of rat Kv7.2/7.3 expressed in CHOK1 cells
|
[PMID: 25987375] |
| CHO-K1 | EC50 |
334 nM
Compound: 2, PF-05020182
|
Activation of human Kv7.2/7.3 expressed in CHOK1 cells
Activation of human Kv7.2/7.3 expressed in CHOK1 cells
|
[PMID: 25987375] |
| CHO-K1 | EC50 |
376 nM
Compound: 2, PF-05020182
|
Activation of rat Kv7.4 expressed in CHOK1 cells
Activation of rat Kv7.4 expressed in CHOK1 cells
|
[PMID: 25987375] |
| CHO-K1 | EC50 |
588 nM
Compound: 2, PF-05020182
|
Activation of human Kv7.3/7.5 expressed in CHOK1 cells
Activation of human Kv7.3/7.5 expressed in CHOK1 cells
|
[PMID: 25987375] |
| CHO-K1 | EC50 |
625 nM
Compound: 2, PF-05020182
|
Activation of human Kv7.4 expressed in CHOK1 cells
Activation of human Kv7.4 expressed in CHOK1 cells
|
[PMID: 25987375] |
| CHO-K1 | EC50 |
>100000 nM
Compound: 2, PF-05020182
|
Activation of human Kv7.1/KCNE1 expressed in CHOK1 cells
Activation of human Kv7.1/KCNE1 expressed in CHOK1 cells
|
[PMID: 25987375] |
Chemical Information
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CAS. Nr. 1354712-92-7
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Molecular Weight 366.46
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Formel C18H30N4O4
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SMILES
O=C(CC(C)(C)C)NC1=C(OC)N=C(N2CCC(CC2)OC)N=C1OC
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)