Home GPCR & G Protein CCR

CCR antagonist/inhibitors

CCR5 is a cell surface beta chemokine receptor. HIV uses CCR5 or CXCR4 as a coreceptor to enter its host cell by binding to a CD4 receptor.Deletion mutation of CCR5 is resistant to HIV-1 infection. Inhibiting human immunodeficiency virus type 1 (HIV-1) infection by blocking the host cell coreceptors CCR5 and CXCR4 is an emerging strategy for antiretroviral therapy.

Other GPCR & G Protein Related Inhibitors

Hedgehog/Smoothened PKA CGRP Receptor Endothelin Receptor S1P Receptor Cannabinoid Receptor SGLT Opioid Receptor GPR MT Receptor

Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S2003 Maraviroc (UK-427857) Maraviroc is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM in cell-free assays, respectively. Maraviroc is used in the treatment of HIV infection.
Nat Commun, 2025, 16(1):4591
Adv Sci (Weinh), 2025, 12(8):e2411711
J Nanobiotechnology, 2025, 23(1):696
Verified customer review of Maraviroc (UK-427857)
S2907 Pirfenidone Pirfenidone is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Pirfenidone attenuates chemokine (CC motif) ligand-2 (CCL2) and CCL12 production with anti-fibrotic activity. Phase 3.
Biomed Pharmacother, 2025, 188:118216
Eur Respir J, 2024, 2300580
Phytomedicine, 2024, 135:156051
Verified customer review of Pirfenidone
S8512 Cenicriviroc Cenicriviroc is a potent, orally active dual inhibitor of CC chemokine receptor 2 (CCR2) and CCR5. This compound also inhibits HIV-1 and HIV-2 with potent anti-inflammatory and antiinfective activity.
Nature, 2025, 10.1038/s41586-024-08535-1
Int J Biol Sci, 2023, 19(8):2572-2587
Stem Cells, 2023, 41(6):672-683
S8220 INCB3344 INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
Biomedicines, 2025, 13(7)1763
MedComm (2020), 2024, 5(5):e535
Commun Biol, 2024, 7(1):488
S2004 Vicriviroc Malate Vicriviroc is a potent CCR5 antagonist with IC50 of 0.91 nM, showing broad-spectrum activity against genetically diverse HIV-1 isolates, and also drug-resistant viruses with RTI, PRI, or MDR phenotypes. Phase 3.
Nature, 2013, 493(7430):51-5
Cancer Res, 2012, 72(15):3839-50
J Antimicrob Chemot, 2011, 66(4):802-12
Verified customer review of Vicriviroc Malate
S0129 SB-297006 SB-297006 is an antagonist of C-C chemokine receptor 3 (CCR3) that suppresses antigen-induced accumulation of T(h)2 as well as eosinophils in the lungs. This compound suppressed CCL11-induced Th2 chemotaxis with IC50 of 2.5 μM.
JHEP Rep, 2023, 5(9):100805
JHEP Rep, 2023, 5(9):100805
Cell Death Dis, 2022, 13(5):478
S8501 Adaptavir (DAPTA) Adaptavir (DAPTA, D-Ala-peptide T-amide, peptide T) is a water soluble potent, selective CCR5 antagonist which potently inhibits specific CD4-dependent binding of gp120 Bal (IC50 = 0.06 nM) and CM235 (IC50 = 0.32 nM) to CCR5.
Cell Death Dis, 2022, 13(5):478
Proc Natl Acad Sci U S A, 2021, 118(9)e2017282118
FEBS J, 2020, 287(11):2367-2385
S8324 ZK756326 2HCl ZK756326 is a full agonist of CCR8（Chemokine receptor 8） with an IC50 of 1.8 μM, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1.
Cancer Immunol Immunother, 2022, 10.1007/s00262-022-03196-3
J Exp Med, 2019, 216(12):2763-2777
S7604 BX471

BX471 (ZK811752, BAY 865047, SH T 04268H) is a potent nonpeptide CC chemokine receptor-1 (CCR1) antagonist with Ki values of 1 nM and 5.5 nM in both MIP-1α and MCP-3 binding to CCR1-transfected HEK293 cells, respectively.
Nat Commun, 2025, 16(1):4581
Commun Biol, 2024, 7(1):1304
S3383 RS102895 RS 102895 is a small molecule antagonist of CCR2 with an IC50 of 360 nM.
Exp Mol Med, 2024, 56(2):408-421.
Theranostics, 2022, 12(17):7351-7370

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