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Cenicriviroc
- TBR 652 - TAK 652 - CVC
- Soluble in DMSO
- MF: C41H52N4O4S
- MW: 696.94
Description
Cenicriviroc (TBR-652, TAK-652, CVC) is an oral, long-acting, dual CCR5 and CCR2 chemokine receptor antagonist, displaying IC50 values of 0.29 nM against CCR5 and 5.9 nM against CCR2.
Cenicriviroc features potent anti-inflammatory and antifibrotic activity, serving as a key research tool across oncology, virology, and immunology models.
Key Features
- Dual Antagonism: Orally bioavailable, long-acting blocker of both CCR2 and CCR5 receptors
- High Potency: Nanomolar inhibition of CCR5 (0.29 nM) and CCR2 (5.9 nM)
- Anti-Inflammatory: Significantly blocks pro-inflammatory monocyte and macrophage infiltration
- Antifibrotic Efficacy: Prevents downstream tissue remodeling and stellate cell activation
Applications
- Fibrosis: Modeling liver, kidney, and lung fibrosis
- Inflammation: Tracking macrophage-driven inflammatory tissue damage
- Oncology: Studying tumor-associated macrophage recruitment and metastasis
- Virology: Profiling CCR5-tropic viral entry and resistance
More Information
| Parent CAS No. | 497223-25-3 |
|---|---|
| Chemical Name | (S)-8-(4-(2-butoxyethoxy)phenyl)-1-isobutyl-N-(4-((1-propyl-1H-imidazol-5-yl)methylsulfinyl)phenyl)-1,2,3,4-tetrahydrobenzo[b]azocine-5-carboxamide |
| MFCD | N.A. |
| Short Description | CCR5 antagonist |
References
- M Baba et al. TAK-652 inhibits CCR5-mediated human immunodeficiency virus type 1 infection in vitro and has favorable pharmacokinetics in humans. Antimicrob Agents Chemother. 2005 Nov;49(11):4584-91.
- M Baba et al. Isolation and Characterization of Human Immunodeficiency Virus Type 1 Resistant to the Small-Molecule CCR5 Antagonist TAK-652. Antimicrob Agents Chemother. 2007 Feb; 51(2): 707–715.
- TJ Henrich et al. HIV-1 entry inhibitors: recent development and clinical use. Curr Opin Virol. 2013 Feb;3(1):51-7.
- M Seto et al. Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety. J Med Chem. 2006 Mar 23;49(6):2037-48.
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