PD 168568
PD 168568 is a orally active and potent dopamine receptor D4 (DRD4) antagonist. PD 168568 contains an isoindolinone and is selective for the D4 receptor versus D2 and D3, with Ki values of 8.8, 1842, and 2682 nM, respectively. PD 168568 can be used for glioblastoma (GBM) research.
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: 210688-56-5
- 分子式: C22H27N3O
- 分子量:349.47
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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
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D4 Receptor 8.8 nM (Ki) |
D2 Receptor 1842 nM (Ki) |
D3 Receptor 2682 nM (Ki) |
体外実験
PD 168568 shows selectivity inhibition toward glioblastoma neural stem cells (GNS), with IC50 of 25-50 µM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rat[1]
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Dosage:3 mg/kg
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Administration:Oral administration
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Result:Inhibited amphetamine (0.5 mg/kg, i.p.) stimulated locomotor activity.
化学情報
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CAS 番号 210688-56-5
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性状 Solid
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分子量 349.47
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分子式 C22H27N3O
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Color White to off-white
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SMILES
O=C1NC(CCN2CCN(C3=CC=C(C)C(C)=C3)CC2)C4=C1C=CC=C4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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データシート (272 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Dolma S, et al. Inhibition of Dopamine Receptor D4 Impedes Autophagic Flux, Proliferation, and Survival of Glioblastoma Stem Cells. Cancer Cell. 2016 Jun 13;29(6):859-873. [Content Brief]
[2]. Lindsley CW, et al. Return of D4 Dopamine Receptor Antagonists in Drug Discovery. J Med Chem. 2017 Sep 14;60(17):7233-7243. [Content Brief]
[3]. Belliotti TR, et al. Isoindolinone enantiomers having affinity for the dopamine D4 receptor. Bioorg Med Chem Lett. 1998 Jun 16;8(12):1499-502. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
PD 168568 関連分類
HY-103407 関連分類
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