VK4-116
VK4-116 (Compound 19) is a selective Dopamine D3 receptor (D3R) antagonist with a Ki of 6.84 nM.VK4-116 significantly inhibits Oxycodone-induced hyperlocomotion and locomotor sensitization in mouse models. VK4-116 with pretreatment also inhibits the acquisition of Oxycodone-induced conditioned place preference (CPP) in rat models.
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: 1982347-43-2
- 分子式: C26H33ClN4O3
- 分子量:485.02
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Dopamine 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
製品説明
IC50 & Target
[1]|
D3 Receptor 6.84 nM (Ki) |
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
>8300 nM
Compound: 19
|
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysis
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysis
|
[PMID: 27508895] |
| CHO | IC50 |
360 nM
Compound: 19
|
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole-stimulated mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysis
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole-stimulated mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysis
|
[PMID: 27508895] |
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1982347-43-2
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分子量 485.02
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分子式 C26H33ClN4O3
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SMILES
O=C(C1=CC2=C(N1)C=CC=C2)NCCC(CN3CCN(CC3)C4=CC(CC)=CC(Cl)=C4OC)O
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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)