AZD-5672

AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM) . AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM) . AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM) . AZD-5672 can be used for the research of rheumatoid arthritis[1][2][3].

Product Specifications

CAS Number

[780750-65-4]

Product Name Alternative

AHPN

UNSPSC

12352005

Target

CCR; P-glycoprotein; Potassium Channel

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Membrane Transporter/Ion Channel

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/azd-5672.html

Purity

95.74

Solubility

DMSO : 33.33 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(N(C1CCN(CC[C@@H](C2=CC(F)=CC(F)=C2)C3=CC=C(S(=O)(C)=O)C=C3)CC1)CC)CC4=CC=C(S(=O)(C)=O)C=C4

Molecular Formula

C32H38F2N2O5S2

Molecular Weight

632.78

References & Citations

[1]Cumming JG, et al. Balancing hERG affinity and absorption in the discovery of AZD5672, an orally active CCR5 antagonist for the treatment of rheumatoid arthritis. Bioorg Med Chem Lett. 2012 Feb 15;22 (4) :1655-9.|[2]Elsby R, et al. The utility of in vitro data in making accurate predictions of human P-glycoprotein-mediated drug-drug interactions: a case study for AZD5672. Drug Metab Dispos. 2011 Feb;39 (2) :275-82.|[3]Gerlag DM, et al. Preclinical and clinical investigation of a CCR5 antagonist, AZD5672, in patients with rheumatoid arthritis receiving methotrexate. Arthritis Rheum. 2010 Nov;62 (11) :3154-60.