CCR5 antagonist 4
CCR5 antagonist 4 is an orally active CCR5 antagonist. CCR5 antagonist 4 can be studied in research on rheumatoid arthritis.
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- CAS. Nr.: 872879-86-2
- Formel: C31H43F2N3O5S2
- Molecular Weight:639.82
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.26 nM
Compound: 7e, AZD-5672
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Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells
Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells
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[PMID: 22266038] |
| HEK293 | IC50 |
24 μM
Compound: 7e, AZD-5672
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Displacement of 3,7-Bis[2-(4-nitro[3,5-3H]phenyl)ethyl]-3,7-diazabicyclo[3.3.1]nonane from human ERG expressed in HEK cells after 3 hrs
Displacement of 3,7-Bis[2-(4-nitro[3,5-3H]phenyl)ethyl]-3,7-diazabicyclo[3.3.1]nonane from human ERG expressed in HEK cells after 3 hrs
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[PMID: 22266038] |
| T-cell | IC50 |
0.69 nM
Compound: 7e, AZD-5672
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Antagonist activity at CCR5 in allo T cells assessed as inhibition of MIP-1beta-induced chemotaxis
Antagonist activity at CCR5 in allo T cells assessed as inhibition of MIP-1beta-induced chemotaxis
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[PMID: 22266038] |
Chemical Information
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CAS. Nr. 872879-86-2
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Molecular Weight 639.82
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Formel C31H43F2N3O5S2
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SMILES
O=C(N(C1CCN(CC[C@@H](C2=CC(F)=CC(F)=C2)C3CCN(S(=O)(C)=O)CC3)CC1)CC)CC4=CC=C(S(=O)(C)=O)C=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Cumming, J. G., et al., (2012). Balancing hERG affinity and absorption in the discovery of AZD5672, an orally active CCR5 antagonist for the treatment of rheumatoid arthritis. Bioorganic & medicinal chemistry letters, 22(4), 1655-1659. [Content Brief]
[2]. Elsby, R., et al., (2011). The utility of in vitro data in making accurate predictions of human P-glycoprotein-mediated drug-drug interactions: a case study for AZD5672. Drug metabolism and disposition: the biological fate of chemicals, 39(2), 275-282. [Content Brief]
[3]. Gerlag, D. M., et al., (2010). Preclinical and clinical investigation of a CCR5 antagonist, AZD5672, in patients with rheumatoid arthritis receiving methotrexate. Arthritis and rheumatism, 62(11), 3154-3160. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
CCR5 antagonist 4 Related Classifications
HY-139184 Related Classifications
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