CCR5 antagonist 4

Cat. No.: HY-139184: Data Sheet Handling Instructions
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CCR5 antagonist 4 is an orally active CCR5 antagonist. CCR5 antagonist 4 can be studied in research on rheumatoid arthritis.

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CCR5 antagonist 4 Chemical Structure

CAS No. : 872879-86-2

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•Related Small Molecules:

•Related Proteins:

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View All Isoforms

CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

Biological Activity
Purity & Documentation
References
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Description

CCR5 antagonist 4 is an orally active CCR5 antagonist. CCR5 antagonist 4 can be studied in research on rheumatoid arthritis^[1]^[2]^[3].

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.26 nM Compound: 7e, AZD-5672	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	[PMID: 22266038]
HEK293	IC₅₀	24 μM Compound: 7e, AZD-5672	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	[PMID: 22266038]
T-cell	IC₅₀	0.69 nM Compound: 7e, AZD-5672	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	[PMID: 22266038]

Molecular Weight

639.82

Formula

C₃₁H₄₃F₂N₃O₅S₂

CAS No.

872879-86-2

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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]