2. Signaling Pathways
  3. GPCR/G Protein
    Immunology/Inflammation
  4. CCR
  5. CCR Antagonist

CCR Antagonist

CCR Isoform Comparison

CCR Antagonists (105):

Cat. No. Product Name Effect Purity
  • HY-144197
    CCR8 antagonist 1
    		Antagonist 99.50%
    CCR8 antagonist 1 (compound 15) is a potente human CCR8 antagonist with a Ki of 1.6 nM.
  • HY-135891
    AZD2423
    		Antagonist 99.91%
    AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca2+ flux .
  • HY-157453
    CCR4 antagonist 4
    		Antagonist 99.72%
    CCR4 antagonist 4 (compound 22) is a selective and potent antagonist of the CC chemokine receptor-4 (CCR4), with an IC50 of 0.02 μM. CCR4 antagonist 4 also blocks MDC-mediated chemotaxis (IC50: 0.007 μM) and Ca2+ mobilization (IC50: 0.003 μM). CCR4 antagonist 4 can be used for allergic inflammation research.
  • HY-156460
    CMKLR1 antagonist 1
    		Antagonist 99.44%
    CMKLR1 antagonist 1 (compound S-26d) is a potent and orally active chemokine-like receptor 1 (CMKLR1) antagonist, with a pIC50 value of 7.44 in hCMKLR1-transfected CHO cells. CMKLR1 antagonist 1 can be used for psoriasis and metabolic diseases research.
  • HY-19974
    TAK-220
    		Antagonist 99.95%
    TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.
  • HY-120427
    Cosalane
    		Antagonist 99.78%
    Cosalane (NSC 658586) is a potent inhibitor of HIV replication. Cosalane has an intrinsic ability to block human and murine CCR7 function in vitro in response to both of its natural ligands, CCL19 and CCL21, with the IC50 of 0.207/2.66 μM in human for CCL19/CCL21 and 0.193/1.98 μM in murine, respectively.
  • HY-103355
    YM022
    		Antagonist 99.93%
    YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo.
  • HY-123763
    MLN3126
    		Antagonist 98.64%
    MLN3126 is an orally active and potent CCR9 antagonist. MLN3126 inhibits CCL25-induced calcium mobilization and chemotaxis of mouse primary thymocytes, wiht an IC50 value of 6.3 nM for calcium influx.
  • HY-U00350
    CCX354
    		Antagonist 99.18%
    CCX354 is an antagonist of CCR1, with anti-inflammatory activity.
  • HY-153670
    IPG7236
    		Antagonist 98.54%
    IPG7236 is a selective CCR8 antagonist. IPG7236 exhibits significant tumor suppression in a mouse xenograft model of human breast cancer. IPG7236 can be used in cancer research.
  • HY-131349
    CCR4-351
    		Antagonist 98.95%
    CCR4-351 is an orally active, potent and selective CCR4 antagonist. CCR4-351, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 has antitumor activity.
  • HY-15546
    BMS-817399
    		Antagonist 99.83%
    BMS-817399 is a potent, selective, and orally bioavailable CCR1 antagonist. BMS-817399 exhibits CCR1 binding affinity and chemotaxis inhibition potencies of 1 and 6 nM (IC50), respectively. BMS-817399 can be used for the research of rheumatoid arthritis.
  • HY-17450A
    Aplaviroc hydrochloride
    		Antagonist 99.94%
    Aplaviroc (AK 602) hydrochloride, a SDP derivative, is a CCR5 antagonist, with IC50s of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL and HIV-1MOKW.
  • HY-109511
    AZD-1678
    		Antagonist 98.12%
    AZD-1678 is a potent CCR4 receptor antagonist, with a pIC50 of 8.6.
  • HY-50669
    MK-0812
    		Antagonist 99.75%
    MK-0812 is a potent and selective CCR2 antagonist with low nM affinity for CCR2.
  • HY-U00331
    CCR3 antagonist 1
    		Antagonist 98.95%
    CCR3 antagonist 1 is a potent antagonist of CCR3, used for the research of immunologic and inflammatory diseases.
  • HY-119101
    AZD-5672
    		Antagonist
    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.
  • HY-101264
    CCR2 antagonist 3
    		Antagonist 99.84%
    CCR2 antagonist 3 is a chemokine receptor 2 (CCR2) antagonist.
  • HY-147385
    CCR4 antagonist 3
    		Antagonist 99.94%
    CCR4 antagonist 3 is a potent chemokine receptor 4 (CCR4) antagonist with an IC50 value of 1.7 μM for [125I]TARC (thymus and activation regulated chemokine). CCR4 antagonist 3 inhibits binding of radiolabeled TARC and macrophage-derived chemokine (MDC) to CCR4 receptors on the surface of CEM cells. CCR4 antagonist 3 also inhibits the in vitro migration of CEM cells mediated by TARC (IC50 = 6.4 μM).
  • HY-131349A
    CCR4-351 hydrochloride
    		Antagonist 98.37%
    CCR4-351 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4-351 hydrochloride, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 hydrochloride has antitumor activity.