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Catalog No.
Product Name
Application
Product Information
Product Citation
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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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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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TLR4 inhibitor
Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor and plays pivotal role in various inflammatory diseases. -
mTOR inhibitor
Zotarolimus is an immunosuppressant. It is a semi-synthetic derivative of rapamycin. It was designed for use in stents with phosphorylcholine as a carrier. - Jaceosidin is a pharmacologically active flavone derived from Artemisia argyi, inhibits phorbol-ester-induced upregulation of COX-2 and MMP-9 by blocking phosphorylation of ERK-1 and -2 in cultured human mammary epithelial cells.
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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. -
HPGDS inhibitor
HPGDS inhibitor 1 is a novel and selective Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50 Value of 0.7 nM. -
CXCL8/CXCR1/2 Inhibitor
Reparixin is a potent inhibitor of both CXCL8 receptors CXCR1/2, it inhibits weakly CXCR2-mediated cell migration (IC50=100 nM), whereas it strongly blocks CXCR1-mediated chemotaxis (IC50=1 nM).- Naour AL, .et al. , J Mol Cell Biol, 2019, Sep 3 PMID: 31504643
- Wigenstam E, .et al. , Toxicology, 2015, Feb 3;328:40-7 PMID: 25497111
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CXCR2 antagonists
CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3. -
TLR8 agonist
VTX-2337 is a small-molecule Toll-like receptor 8 (TLR8) agonist with potential immunostimulating and antineoplastic activities.- Yinwen Cheng, .et al. , Sci Rep, 2021, Jan 15;11(1):1535 PMID: 33452311
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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. - 21-Deacetoxy Deflazacort is an intermediate of Deflazacort, a systematic corticosteroid.
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NOS cofactor
Biopterin is the oxidized form of tetrahydro-L-biopterin (BH4), a nitric oxide synthase (NOS) cofactor. L-Biopterin can be reduced to BH4 via thioredoxin reductase followed by dihydropteridine reductase or reduced glutathione. It is extremely toxic to human melanocytes in culture (IC50 = 0.2 uM after 48 hrs). -
Thrombopoietin(TPO) receptor agonist
Avatrombopag is a novel orally-active thrombopoietin (TPO) receptor agonist. -
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. -
CXCL8 receptor inhibitor
Reparixin L-lysine salt is an inhibitor of CXCL8 receptor, also inhibit CXCR1 and CXCR2 activation,which has been shown to attenuate inflammatory responses in various injury models. - Toll-like receptors (TLRs) are a class of proteins that play a key role in the innate immune system.
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CCR5 antagonist
Vicriviroc maleate is a CCR5 antagonist with IC50 of 0.91 nM in clinical development for the treatment of HIV-1. -
Calcineurin inhibitor
Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation. -
Calcineurin/PP2B inhibitor
Ascomycin is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties. It has been researched for the treatment of autoimmune diseases and skin diseases, and to prevent rejection after an organ transplant. -
PD-1/PD-L1 interaction inhibitor
PD-1/PD-L1 inhibitor 2 is a PD-1/PD-L1 interaction inhibitor. -
COX inhibitor
Diflunisal is a salicylic acid derivative with analgesic and anti-inflammatory activity. -
TPO agonist
TPO agonist 1 can increase production of platelets by stimulating the TPO receptor in people with chronic ITP. - Prostaglandin F2α is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient.
- Michel R Corboz, .et al. , Prostaglandins Other Lipid Mediat, 2020, Oct 1;152:106486 PMID: 33011365
