Carlumab (CNTO 888) is a humanised anti-CCL2 (chemokine ligand 2) antibody with high affinity. Carlumab can be used in cancer research, particularly in prostate cancer[1].
PMX53 (Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg)) is a potent C5a receptor (CD88) antagonist with IC50 of 20 nM, also is an agonist for Mas-related gene 2 (MrgX2) in human mast cells; PMX-53 (10 nM) inhibited C5a-induced Ca(2+) mobilization in HMC-1 cells, but at higher concentrations (>30 nM) it caused degranulation in LAD2 mast cells, CD34(+) cell-derived mast cells, and RBL-2H3 cells stably expressing MrgX2; inhibits zymosan-, carrageenan-, LPS- and antigen-induced hypernociception in rats.
FC131 TFA 是一种 CXCR4 拮抗剂，抑制 [125I]-SDF-1 与 CXCR4 结合，IC50 值为 4.5 nM。FC131 TFA 具有抗 HIV 的活性。
CL656 is an activator of stimulator of interferon genes (STING).
AHR antagonist 5 free base is a selective and orally active aryl hydrocarbon receptor (AHR) inhibitor. AHR antagonist 5 free base effectively blocks AHR from translocating from the cytoplasm to the nucleus. AHR antagonist 5 free base is highly selective for AHR over other receptors, transporters, and kinases[1].
Vadimezan (ASA-404; DMXAA), the vascular disrupting agent, is a murine agonist of the stimulator of interferon genes (STING) and also a potent inducer of type I IFNs and other cytokines.
BMS-753426 is a potent and orally bioavailable antagonist of CCR2.
Maceneolignan H (Compound 8) is a neolignane compound isolated from the arils of Myristica fragrans. Maceneolignan H is a selective CCR3 antagonist (EC50 = 1.4 μM). Maceneolignan H has the potential for the research of allergic diseases[1].
AL-8417 is an enzyme inhibitor. It acting as an antioxidant, anti-inflammatory, and cytostatic agent. It also has the ability to suppress vitrectomy-induced posterior lens fiber changes.
Moracin C, a natural product, is an anti-inflammatory agent. Moracin C inhibits LPS-activated reactive oxygen species (ROS) and nitric oxide (NO) release from cells[1].
ODN M326 (CpG-ODN M326) is a potent TLR9 agonist. ODN M326 induces the production of TNF. ODN M326 can be used as a vaccine adjuvant[1].
6-Methoxynaringenin is a natural flavonoid that inhibits NO production with an IC50 of 25.8 μM[1].
Rupatadine (UR-12592) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in human platelet-rich plasma (HPRP) (IC50 = 0.68 microM), while not affecting ADP- or arachidonic acid-induced platelet aggregation [1]. The IC50 for rupatadine in A23187, concanavalin A and anti-IgE induced histamine release was 0.7+/-0.4 microM, 3.2+/-0.7 microM and 1.5+/-0.4 microM, respectively whereas for loratadine the IC50 was 2.1+/-0.9 microM, 4.0+/-1.3 M and 1.7+/-0.5 microM. SR-27417A exhibited no inhibitory effect [2].in vivo: Rupatadine blocked histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID50 = 1.4 and 0.44 mg/kg i.v., respectively) and bronchoconstriction in guinea pigs (ID50 = 113 and 9.6 micrograms/kg i.v.). Moreover, it potently inhibited PAF-induced mortality in mice (ID50 = 0.31 and 3.0 mg/kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID50 = 1.6 and 0.66 mg/kg i.v.) [1]. rupatadine treatment improved the declined lung function and significantly decreased animal death. Moreover, rupatadine was able not only to attenuate silica-induced silicosis but also to produce a superior therapeutic efficacy compared to pirfenidone, histamine H1 antagonist loratadine, or PAF antagonist CV-3988 [3].
Phenylbutazone-d10 (diphenyl) is the deuterium labeled Phenylbutazone. Phenylbutazone is an efficient reducing cofactor for the peroxidase activity of prostaglandin H synthase (PHS). Phenylbutazone, a hepatotoxin, is a nonsteroidal anti-inflammatory drug (NSAID). Phenylbutazone induces muscle blind-like protein 1 (MBNL1) expression and has the potential for ankylosing spondylitis research[1][2].
Pectolinarigenin, isolated from Cirsium chanroenicum, is a dual inhibitor of COX-2/5-LOX. Anti-inflammatory activity[1]. Pectolinarigenin has potent inhibitory activities on melanogenesis[2].
Pam2CSK4, a lipopeptide, is a TLR6-independent TLR2 ligand and agonist. Pam2CSK4 promotes platelet aggregation, and increases platelet adhesion to collagen-coated surfaces in a TLR2/NF-κB/BTK-dependent manner. Pam2CSK4 also activates iNOS expression and NO production in mouse macrophages[1][2][3].
Cenicriviroc is an orally active, dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.
M-TriDAP (N-Acetylmuramyl-L-Ala-γ-D-Glu-meso-diaminopimelic acid) is a biological active peptide. (NOD1/2 Agoist)
PD-1/PD-L1-IN-32 (compound A56) is a potent PD-1/PD-L1 inhibitor (IC50=2.4 nM), with anticancer activity. PD-1/PD-L1-IN-32 significantly inhibits tumor growth in hPD-L1 MC38 humanized mouse model, without obvious toxicity against mouse normal ability[1].
Asperuloside is an iridoid isolated from Hedyotis diffusa, with anti-inflammatory activity. Asperuloside inhibits inducible nitric oxide synthase (iNOS), suppresses NF-κB and MAPK signaling pathways[1].
Remtolumab (ABT-122) is a dual-variable domain immunoglobulin that neutralises both tumor necrosis factor α (TNFα) and IL-17A. Remtolumab shows dual inhibition of TNFα and IL-17A. Remtolumab can be used for rheumatoid arthritis (RA) research[1][2].
NIC-0102 is an orally active proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammatory vesicle activation. NIC-0102 shows potent anti-inflammatory effects in a model of dextran sulfate sodium (DSS)-induced ulcerative colitis. NIC-0102 also inhibits production of pro-IL-1β[1].
NDT 9513727 is a potent, selective, orally active and competitive inverse agonist of the human C5aR (C5a receptor), with an IC50 of 11.6 nM. NDT 9513727 can be used for the research of human inflammatory diseases[1].
C-021 dihydrochloride is a potent and orally bioavailable CCR4 antagonist with IC50 of 0.14 uM and 0.039 uM for inhibition of chemotaxis in human and mouse, respectively.
Rolinsatamab is a potent dual IL-4 and IL-13 inhibitor as a fully humanized bispecific monoclonal antibody. Rolinsatamab chimeric antigen receptor sequence T cell. Rolinsatamab can be used in research of immune disease[1].
Lusvertikimab (OSE-127) is a humanized IL7R monoclonal antibody. Lusvertikimab is not internalized by target cells and prevents IL7R heterodimerization and subsequent downstream signaling. Lusvertikimab has anti-leukemic efficacy and has the potential for B cell precursor acute lymphoblastic leukemia (BCP-ALL) research[1].
JT001 (NLRP3-IN-19) is a potent, specific and orally active inhibitor of NLRP3. JT001 can inhibit NLRP3 inflammasome assembly, resulting in the inhibition of cytokine release and the prevention of pyroptosis. JT001 can be used for the research of nonalcoholic steatohepatitis and liver fibrosis[1].
Polyinosinic acid is a single stranded homonucleic acid, which is a Toll-like Receptor 3 (TLR3) agonist. Polyinosinic acid enhances cellular immune response through TLR3 and TRIF. Polyinosinic acid has potential applications in immune regulation[1].
Limaprost-d3 (17α,20-dimethyl-δ2-PGE1-d3) is the deuterium labeled Limaprost. Limaprost (OP1206) is a PGE1 analogue and a potent and orally active vasodilator. Limaprost increases blood flow and inhibits platelet aggregation. Limaprost pain relief, has antianginal effects, and can be used for ischaemic symptoms research[1][2].
Bepotastine tosylate is a selective and orally active second-generation histamine H1 receptor antagonist. Bepotastine tosylate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research[1][2][3].