JJC8-088
JJC8-088, a Modafinil-derived ligand, is a dopamine transporter (DAT) inhibitor with a Ki of 2.53 nM. JJC8-088 dioxalate can be to study psychostimulant use disorders.
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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: 1627576-82-2
- 分子式: C28H32F2N2O2S
- 分子量:498.63
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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DAT 2.53 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
>10000 nM
Compound: 11b, JJC 8-088
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Antagonist activity at DRD2 (unknown origin) expressed in HEK293T cells transfected with Galphai1-RLuc8 and gamma2-GFP10 assessed as inhibition of quinpirole-induced Gi1 activation pre-incubated with quinpirole for 10 mins before compound incubation for 1
Antagonist activity at DRD2 (unknown origin) expressed in HEK293T cells transfected with Galphai1-RLuc8 and gamma2-GFP10 assessed as inhibition of quinpirole-induced Gi1 activation pre-incubated with quinpirole for 10 mins before compound incubation for 1
|
[PMID: 27933960] |
JJC8-088 (0-30 mg/kg, i.p., 30 min prior to testing) can cause a large and rapid increase in extracellular Dopamine (DA) (HY-B0451) levels in rats with history of toxic molecules self-administration[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:METH addict male Wistar rats (6-8 weeks old; weighing 200-250 g)[1].
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Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:i.p.
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Result:The half-life was 39 min.
Presented low levels in both brain and plasma.
化学情報
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CAS 番号 1627576-82-2
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分子量 498.63
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分子式 C28H32F2N2O2S
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SMILES
O=S(C(C1=CC=C(C=C1)F)C2=CC=C(C=C2)F)CCN3CCN(CC3)CC(CC4=CC=CC=C4)O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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
[1]. Tunstall BJ, et al. Atypical dopamine transporter inhibitors attenuate compulsive-like methamphetamine self-administration in rats. Neuropharmacology. 2018 Mar 15;131:96-103. [Content Brief]
[2]. Newman AH, et al. Translating the atypical dopamine uptake inhibitor hypothesis toward therapeutics for treatment of psychostimulant use disorders. Neuropsychopharmacology. 2019 Jul;44(8):1435-1444. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)