DNK-333
DNK-333 is a potent and balanced dual NK1 and NK2 receptor antagonist with IC50 values of 4.8 nM and 5.5 nM, respectively. DNK-333 blocks the Neurokinin A (NKA) (HY-P0197)-induced bronchoconstriction in asthma.
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: 398507-81-8
- 分子式: C27H25Cl2F6N3O3
- 分子量:624.40
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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
生物活性
製品説明
IC50 & Target
[1]|
NK1R 9.2 (pkB) |
NK2R 7.43 (pkB) |
hNK1 4.8 nM (IC50) |
hNK2 5.5 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
5.5 nM
Compound: 9 (DNK333)
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In vitro binding affinity for Tachykinin receptor 2 of human-CHO cells using 125 I-NKA radioligand
In vitro binding affinity for Tachykinin receptor 2 of human-CHO cells using 125 I-NKA radioligand
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[PMID: 11714615] |
体外実験
DNK-333 exhibits potent and reversible NK1 and NK2 receptor antagonist activities in this assay, with pKb values of 9.2 and 7.43, respectively[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.
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 398507-81-8
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分子量 624.40
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分子式 C27H25Cl2F6N3O3
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SMILES
O=C(N([C@H](CC1=CC(Cl)=C(Cl)C=C1)/C=C/C(N[C@H]2C(NCCCC2)=O)=O)C)C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3
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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]. Swarna VM, et al. Design and synthesis of 3,5-disubstituted benzamide analogues of DNK333 as dual NK1/NK2 receptor probes. Bioorg Med Chem Lett. 2007 Feb 15;17(4):890-4. [Content Brief]
[2]. Schelfhout V, et al. The triple neurokinin-receptor antagonist CS-003 inhibits neurokinin A-induced bronchoconstriction in patients with asthma. Pulm Pharmacol Ther. 2006;19(6):413-8. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
DNK-333 関連分類
HY-128537 関連分類
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