BMS-570520
BMS-570520 is an orally bioavailable CCR3 antagonist with an IC50 of 1.9 nM against hCCR3 and an IC50 of 1300 nM against hCYP2D6. BMS-570520 inhibits CYP2D6, but shows low activity against off-target G protein-coupled receptors, biogenic amine transporters, and the hERG potassium channel. BMS-570520 regulates chemotaxis, calcium mobilization, and anti-inflammatory pathways. BMS-570520 can be used in research related to asthma, allergic rhinitis, and contact dermatitis.
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: 388101-58-4
- 分子式: C27H36FN5O3S
- 分子量:529.67
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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
- プロトコル
- 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
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CCR3 1.9 nM (IC50) |
CYP2D6 1.3 |
5-HT2A Receptor 5.3 μM (IC50) |
D2 Receptor 0.64 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1.9 nM
Compound: 8i
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Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
Displacement of [125I]eotaxin from human CCR3 expressed in CHO cells after 30 mins
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[PMID: 17418570] |
体外実験
BMS-570520 inhibits the binding of eotaxin to human CCR3 and mouse CCR3, with IC50 values of 1.9 nM and 3.6 nM, respectively[1].
BMS-570520 inhibits eotaxin-induced chemotaxis of human eosinophils or mouse eosinophils, with IC50 values of 0.068 nM and 7 nM, respectively[1].
BMS-570520 inhibits eosinophil chemokine-induced calcium mobilization via human CCR3, with an IC50 of 2.6 nM[1].
BMS-570520 exhibits off-target activity against human 5HT2A (IC50=5300 nM), D2 (IC50=640 nM), hERG (IC50=6000 nM), serotonin transporter (Ki=29,000 nM), dopamine transporter (Ki=6500 nM), and norepinephrine transporter (Ki=7700 nM)[1].
The apparent permeability coefficient of BMS-570520 in human Caco-2 cells is 2.8 × 10-6 cm/s[1].
BMS-570520 exhibits a protein binding rate of 93.1% in human serum and an intrinsic clearance of 0.96 L/h/kg in human liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 388101-58-4
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分子量 529.67
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分子式 C27H36FN5O3S
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SMILES
CC(C(SC(NC(N[C@H](CN(CC1)C(C)=O)[C@@H]1CN2C[C@@H](CCC2)CC3=CC=C(C=C3)F)=O)=N4)=C4C)=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
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
BMS-570520 関連分類
HY-182735 関連分類
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Keywords
- BMS-570520
- 388101-58-4
- BMS570520
- BMS 570520
- CCR
- Cytochrome P450
- 5-HT Receptor
- Dopamine Receptor
- Serotonin Transporter
- G protein-coupled receptors
- anti-inflammatory pathways
- human CCR3
- asthma
- calcium mobilization
- hERG potassium channels
- allergic rhinitis
- human CYP2D6
- chemotaxis
- biogenic amine transporters
- Inhibitor
- inhibitor
- inhibit