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Catalog No.
Product Name
Application
Product Information
Product Citation
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S1P Receptor antagonist
FTY720 is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb Iscaria sinclarii as well as a structural analog of sphingosine.- Tina Sepasi, .et al. , Int J Pharm, 2023, Apr 5;636:122815 PMID: 36907279
- Tina Sepasi, .et al. , BioImpacts, 2022, 28 May
- Zengzi Zhou, .et al. , Infect Immun, 2020, Oct 19;88(11):e00281-20 PMID: 32868341
- Mayu Idehara, .et al. , Traditional & Kampo Medicine, 2020, 22 July
- Luwa Yuan, .et al. , Sci Rep, 2019, 9:11156 PMID: 31371790
- Sakai Y, .et al. , Int J Biol Macromol, 2018, Nov 22;124:505-514 PMID: 30471397
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CCR antagonist
Maraviroc is an antiretroviral drug in the CCR5 receptor antagonist class used in the treatment of HIV infection.- Roman V Uzhachenko, .et al. , Cell Rep, 2021, Apr 6;35(1):108944 PMID: 33826903
- Karampoor S, .et al. , Int Immunopharmacol, 2020, Mar;80:106138 PMID: 32007705
- Taisuke Ito, .et al. , JCIA, 2020, 22 January
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CXCR4 antagonist
Plerixafor is an immunostimulant used to multiply hematopoietic stem cells and it is a chemokine receptor-4 antagonist for mobilization of hematopoietic stem cells for transplantation.- Federico Antoniciello, .et al. , Front Mol Biosci, 2023, May 11;9:887564 PMID: 35647033
- Mei Zheng, .et al. , Biomed Pharmacother, 2022, Jun;150:112996 PMID: 35462338
- Asiedu KO, .et al. , EJNMMI Res, 2018, Dec 13;8(1):109 PMID: 30547233
- Kingsley O. Asiedu, .et al. , Clin Cancer Res, 2017, Jun 1; 23(11): 2759-2768 PMID: 27965305
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CCR5 antagonist
Vicriviroc Malate is a second generation orally active CCR5 antagonist, which is also a potent inhibitor of HIV-1 entry into target cells, with a mean IC50 =0.46 nM and IC50 =1~10 nM to HIV isolates (n=52).- Tomohiro Nabekura, .et al. , Antimicrob Agents Chemother, 2015, Dec; 59(12): 7666-7670 PMID: 26416870
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HCCR2 antagonist
INCB 3284 dimesylate is a potent, selective hCCR2 antagonist that exhibits potenct antagonism against monocyte chemoattractant molecule binding to hCCR2 and chemotaxis activity. -
CCR2 antagonist
MK-0812 is a potent and selective CCR2 antagonist with low nM affinity for CCR2 on human monocytes and low nM in the chemotaxis assay. It has good PK profiles in preclinical species and demonstrated efficacy in animal models.- Murakami K, .et al. , Vet Immunol Immunopathol, 2016, Dec;182:52-58 PMID: 27863550
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CCR2 Antagonist
INCB8761(PF-4136309) is a potent, selective, and orally bioavailable CCR2 antagonist. -
CXCR4 antagonist
AMD 070 is a CXCR4 chemokine receptor antagonist.- Uchida D, .et al. , Oncol Rep, 2018, Jul;40(1):303-308 PMID: 29749473
- Mamoru Morimoto, .et al. , BMC Cancer, 2016, 16: 305 PMID: 27175473
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CXCR1/CXCR2 antagonist
SCH527123 is a potent and selective antagonist of the human CXCR1 and CXCR2 receptors with IC50 of 42 nM and 3 nM, respectively.- Ruijie Zhang, .et al. , Int J Oncol, 2022, May;60(5):50 PMID: 35315502
- Fu S, .et al. , Int J Oncol, 2018, Jul;53(1):349-357 PMID: 29749433
- Fu S, .et al. , Anticancer Res, 2018, Nov;38(11):6271-6279 PMID: 30396947
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CXCR4 antagonist
AMD 3465 is a potent, selective CXCR4 antagonist.- Kentaro Suzuki, .et al. , Sci Rep, 2019, 9: 15284
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CCR4 antagonist
GSK2239633A is a CC-chemokine receptor 4 (CCR4) antagonist, which inhibits the binding of [125I]-TARC to human CCR4 with a pIC50 of 7.96??0.11. -
CXCR2 antagonists
CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3. -
CXCR4 antagonist
Plerixafor is an immunostimulant used to multiply hematopoietic stem cells and it is a chemokine receptor-4 antagonist for mobilization of hematopoietic stem cells for transplantation.- Hitoshi Maeda, .et al. , Int J Biol Macromol, 2022, Sep 17;221:1439-1452 PMID: 36126807
- Jingying Chen, .et al. , Development, 2022, Jul 1;149(13) PMID: 35694896
- Narubhorn Ongprakobkul, .et al. , Am J Orthod Dentofacial Orthop, 2022, Mar 2;S0889-5406(22)00107-X PMID: 35248418
- Chunliang Liu, .et al. , J Trace Elem Med Biol, 2022, Jan 10;71:126927 PMID: 35030482
- Eri Watanabe, .et al. , Angiogenesis, 2020, Jul 22 PMID: 32699964
- Alessandra Esposito, .et al. , Bone, 2020, Jul 3;139:115521 PMID: 32629173
- Kentaro Suzuki, .et al. , Sci Rep, 2019, 9: 15284
- Ichimizu S, .et al. , J Control Release, 2019, May 10;304:156-163 PMID: 31082432
- Nan Li, .et al. , Diagn Pathol, 2019, Jan 12;14(1):3 PMID: 30636642
- Thida W, .et al. , Biochem Biophys Res Commun, 2018, Nov 20. pii: S0006-291X(18)32477-X PMID: 30470571
- Henry R. Hampton, .et al. , Nat Commun, 2015, 6: 7139 PMID: 25972253
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CCR 2 antagonist
Teijin compound 1 is a specific CCR 2 antagonist with IC50s of 24 and 180 nM in chemotaxis and binding assay, respectively. -
CXCR2 antagonist
SB 265610 is a nonpeptide, allosteric, inverse agonist of CXCR2 (Kd = 2.51 nM) that prevents receptor activation by binding to a region distinct from the agonist binding site. It does not bind to the related CXCR1 receptor.1 It has been shown to prevent neutrophil chemotaxis both in vitro and in a rat model of hyperoxia-induced lung injury. -
CXCR4 antagonist
AMD-070 hydrochloride is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, inhibit the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs. -
CCR2 antagonist
PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2. -
CXCR2/CXCR1 antagonist
SCH 563705 is a potent dual CXCR2(IC50= 1.3 nM)/CXCR1(IC50= 7.3 nM) antagonist. -
CCR5 antagonist
Vicriviroc maleate is a CCR5 antagonist with IC50 of 0.91 nM in clinical development for the treatment of HIV-1. -
interleukin-5 receptor antagonist
YM-90709 is an interleukin-5 receptor antagonist. YM-90709 inhibits the binding of IL-5 to its receptor on peripheral human eosinophils and butyric acid-treated eosinophilic HL-60 clone 15 cells, with IC50 values of 1.0 and 0.57 microM, respectively. -
CCR2/CCR5 antagonist
BMS-813160 is a potent and selective CCR2/CCR5 antagonist with potential immunomodulating and antineoplastic activities. -
Acid pump antagonist
Revaprazan hydrochloride is a novel acid pump antagonist (APA). Revaprazan hydrochloride reduces COX-2 expression and has significant anti-inflammatory actions activities in H. pylori infection. -
S1P antagonist
Fingolimod is a sphingosine 1-phosphate (S1P) antagonist with IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant. -
thromboxane A2 (TXA2) receptor (TP receptor) antagonist
Seratrodast is a thromboxane A2 (TXA2) receptor (TP receptor) antagonist used primarily in the treatment of asthma. -
CCR4 antagonist
CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. -
CCR2 /CCR5 dual antagonist
PF-04634817 is an orally administered CCR2 and CCR5 chemokine receptor antagonist, for the treatment of diabetic nephropathies and diabetic macular oedema. -
CCR2 antagonist
CCR2 antagonist 1 is a high-affinity and long-residence-time CCR2 antagonist, with a Ki of 2.4 nM.
