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.
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- CAS No.: 388101-58-4
- Formule: C27H36FN5O3S
- Masse moléculaire:529.67
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Activité biologique
Description
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 |
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| 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] |
In Vitro
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.
Chemical Information
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CAS No. 388101-58-4
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Masse moléculaire 529.67
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BMS-570520 Related Classifications
HY-182735 Related Classifications
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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