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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1354712-92-7
- 分子式: C18H30N4O4
- 分子量:366.46
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
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] |
化学情報
-
CAS 番号 1354712-92-7
-
分子量 366.46
-
分子式 C18H30N4O4
-
SMILES
O=C(CC(C)(C)C)NC1=C(OC)N=C(N2CCC(CC2)OC)N=C1OC
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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
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)