PF-03246799
PF-03246799 is a potent and selective 5-HT2C receptor agonist with an EC50 of 190 nM and a Ki of 160 nM. PF-03246799 shows selectivity for 5-HT2C over 5-HT2A and 5-HT2B receptors. PF-03246799 has the potential for stress urinary incontinence (SUI) research.
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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: 1065110-62-4
- 分子式: C15H17N3
- 分子量:239.32
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
5-HT Receptor アイソフォーム固有の製品をすべて表示
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生物活性
|
5-HT2C Receptor 190 nM (EC50) |
5-HT2C Receptor 160 nM (Ki) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
4.5 nM
Compound: 7b, PF-3246799
|
Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
|
[PMID: 21195614] |
| NIH3T3 | EC50 |
190 nM
Compound: 7b, PF-3246799
|
Agonist activity at human 5HT2C receptor expressed in Swiss mouse 3T3 cells with low expression increase of fluorescence based calcium mobilization by FLIPR assay
Agonist activity at human 5HT2C receptor expressed in Swiss mouse 3T3 cells with low expression increase of fluorescence based calcium mobilization by FLIPR assay
|
[PMID: 21195614] |
| NIH3T3 | EC50 |
4.5 nM
Compound: 7b, PF-3246799
|
Agonist activity at human 5HT2C receptor highly expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay
Agonist activity at human 5HT2C receptor highly expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay
|
[PMID: 21195614] |
| NIH3T3 | EC50 |
68 nM
Compound: 7b, PF-3246799
|
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay
|
[PMID: 21195614] |
化学情報
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CAS 番号 1065110-62-4
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分子量 239.32
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分子式 C15H17N3
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SMILES
C12=NC(CC3=CC=CC=C3)=NC=C1CCNCC2
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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)