CCR5 antagonist 4
CCR5 antagonist 4 is an orally active CCR5 antagonist. CCR5 antagonist 4 can be studied in research on rheumatoid arthritis.
For research use only. We do not sell to patients.
- CAS No.: 872879-86-2
- Formula: C31H43F2N3O5S2
- Molecular Weight:639.82
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Storage:
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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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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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 No. 872879-86-2
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Molecular Weight 639.82
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Collagen-Induced Arthritis
Collagen-induced arthritis (CIA) is an autoimmune murine model of rheumatoid arthritis in which immunization with type II collagen (CII) emulsified in an adjuvant induces a T cell- and autoantibody-driven inflammatory arthritis characterized by synovial hyperplasia, immune cell infiltration, and joint destruction. The model typically relies on genetically susceptible mouse strains (e. g. , DBA/1) and reproduces key features of human rheumatoid arthritis, including anti-collagen immune responses and progressive joint inflammation. Disease onset generally occurs within ~3-4 weeks after immunization, depending on antigen/adjuvant combinations and protocol variation. The immunopathology is driven by adaptive immune activation against CII, leading to systemic and local joint inflammation mediated by pro-inflammatory cytokines and effector immune cells, making CIA a standard preclinical platform for evaluating immunomodulatory and anti-arthritic interventions.
Purity & Documentation
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CCR5 antagonist 4 Related Classifications
HY-139184 Related Classifications
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