Atagabalin
Atagabalin (PD 0200390) is a Voltage-gated Calcium channel α2δ subunit binder with an IC50 of 22 nM. Atagabalin regulates neurotransmitter release by inhibiting calcium influx at high neuronal firing rates. Atagabalin can be used in research related to sleep disorders.
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: 223445-75-8
- 分子式: C10H19NO2
- 分子量:185.26
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
Calcium Channel 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
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Calcium Channel |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
10 μM
Compound: 5
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Inhibition of L-type amino acid transporter expressed in CHO cells assessed as inhibition of [3H]leucine uptake
Inhibition of L-type amino acid transporter expressed in CHO cells assessed as inhibition of [3H]leucine uptake
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[PMID: 20005103] |
Atagabalin potently binds to the VGCC α2δ subunit with an IC50 of 22 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 223445-75-8
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分子量 185.26
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分子式 C10H19NO2
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SMILES
O=C(O)CC1(CN)C[C@H](C)[C@@H](C)C1
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別名
PD 0200390
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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]. Kjellsson MC, et al. Modeling sleep data for a new drug in development using markov mixed-effects models. Pharmaceutical research. 2011 Oct;28(10):2610-27. [Content Brief]
[2]. Corrigan B, et al. Effect of renal impairment on the pharmacokinetics of PD 0200390, a novel ligand for the voltage-gated calcium channel alpha-2-delta subunit. British journal of clinical pharmacology. 2009 Aug;68(2):174-80. [Content Brief]
[3]. Chen Y, et al. Review of Voltage-gated Calcium Channel α2δ Subunit Ligands for the Treatment of Chronic Neuropathic Pain and Insight into Structure-activity Relationship (SAR) by Pharmacophore Modeling. Current medicinal chemistry. 2022 Aug 15;29(30):5097-5112. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Atagabalin 関連分類
HY-14856 関連分類
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- Atagabalin
- 223445-75-8
- PD 0200390
- PD0200390
- PD-0200390
- Calcium Channel
- renal excretion
- neurotransmitter release
- calcium channel α2δ subunit
- insomnia
- sleep disturbance
- slow-wave sleep
- rapid eye movement sleep
- pharmacophore modeling
- voltage-gated calcium channel alpha-2-delta subunits
- calcium influx
- Inhibitor
- inhibitor
- inhibit