E913

E913 is a CCR5 antagonist that competes with the binding of antibodies to CCR5 which recognize the C-terminal half of the second extracellular loop (ECL2B) of CCR5. E913 can specifically block the binding of macrophage inflammatory protein-1alpha (MIP-1alpha) to CCR5 (IC50 = 0.002 μM) and MIP-1alpha-elicited cellular Ca2+ mobilization (IC50 = 0.02 μM) . E913 inhibits the replication of laboratory and primary R5 HIV-1 strains as well as various multidrug-resistant monocyte/macrophage tropic (R5) HIV-1 (IC50 = 0.03-0.06 μM) . E913 can be used for the research of infection, such as HIV-1 infection[1].

Product Specifications

CAS Number

[342394-93-8]

UNSPSC

12352005

Target

CCR; HIV

Related Pathways

Anti-infection; GPCR/G Protein; Immunology/Inflammation

Applications

COVID-19-anti-virus

Field of Research

Infection

Smiles

O=C(N(C12CCN(CC1)CC3=CC=C4OCCOC4=C3)CCCC)C(NC2=O)CC5CCCCC5

Molecular Formula

C28H41N3O4

Molecular Weight

483.64

References & Citations

[1]Maeda K, et al. Novel low molecular weight spirodiketopiperazine derivatives potently inhibit R5 HIV-1 infection through their antagonistic effects on CCR5. J Biol Chem. 2001 Sep 14;276 (37) :35194-200.