TAK-779

TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.

Product Specifications

CAS Number

[229005-80-5]

Product Name Alternative

Takeda 779

UNSPSC

12352005

Target

CCR; CXCR; HIV

Type

Reference compound

Related Pathways

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

Applications

COVID-19-anti-virus

Field of Research

Infection; Inflammation/Immunology; Endocrinology

Assay Protocol

https://www.medchemexpress.com/TAK-779.html

Purity

99.89

Solubility

DMSO : ≥ 25 mg/mL|H2O : 16.66 mg/mL (ultrasonic; warming)

Smiles

C[N+](C)(CC1=CC=C(NC(C2=CC3=CC(C4=CC=C(C)C=C4)=CC=C3CCC2)=O)C=C1)C5CCOCC5.[Cl-]

Molecular Formula

C33H39ClN2O2

Molecular Weight

531.13

References & Citations

[1]Baba M, et al. A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity. Proc Natl Acad Sci U S A. 1999 May 11;96 (10) :5698-703.|[2]Takama Y, et al. Effects of a calcineurin inhibitor, FK506, and a CCR5/CXCR3 antagonist, TAK-779, in a rat small intestinal transplantation model. Transpl Immunol. 2011 Jul;25 (1) :49-55.|[3]Ni J, et al. The chemokine receptor antagonist, TAK-779, decreased experimental autoimmune encephalomyelitis by reducing inflammatory cell migration into the central nervous system, without affecting T cell function. Br J Pharmacol. 2009 Dec;158 (8) :2046-56.|[4]Gao P, et al. The unique target specificity of a nonpeptide chemokine receptor antagonist: selective blockade of two Th1 chemokine receptors CCR5 and CXCR3. J Leukoc Biol. 2003 Feb;73 (2) :273-80.