Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II)[1][2].
IX 207-887 is a novel antiarthritic agent which inhibits the release of interleukin-1 (IL-1).
Beraprost sodium, a prostacyclin analog, is a stable and orally active prodrug of PGI2. Beraprost sodium is a potent vasodilator, has the potential for pulmonary arterial hypertension treatment through expanding renal vessels, improving microcirculation[1].
FR183998 free base is a potent Na+/H+-exchange inhibitor, with IC50s of 0.3 nM, 3.1 nM and 6.5 nM by measurement of pHi change in rat lymphocytes, rat and human platelets, respectively.
Ro 24-5913 (Cinalukast) is an orally active and potent LTD4 antagonist with an IC50 value of 6.4 nM. Ro 24-5913 can be used for the research of asthma[1].
γ-Globulins from human blood are a class of proteins in the blood. γ-Globulin is a protein fraction of blood serum containing many antibodies that protect against bacterial and viral infectious diseases. γ-Globulins from human blood is used for common variable immunodeficiency[1][2]
IRAK4-IN-10 (compound 75) is a potent IRAK4 inhibitor with an IC50 of 1.5 nM. IRAK4-IN-10 blocks MyD88 dependent signaling. IRAK4-IN-9 has the potential for the research of inflammatory diseases, autoimmune diseases, and cancer[1].
Iα52 is a naturally processed peptide encompassed the residues 52-68 of the murine I-Eα chain and may contribute to selection of immature T cells[1].
Cetirizine Impurity C dihydrochloride is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist[1][2].
Oxothiazolidinecarboxylic acid, an antioxidant, is a prodrug of cysteine that is inert until metabolized to cysteine intracellulary, thus stimulating glutathione synthesis[1].
MRS 1754 is a selective antagonist radioligand for A2B adenosine receptor with very low affinity for A1 and A3 receptors of both humans and rats[1].
Belatacept (BMS 224818) is a selective T-cell costimulation blocker. Belatacept binds to CD 80/86 ligands and thereby inhibits the CD-28-mediated T-cell costimulation. Belatacept can be used in the research of Immunosuppression in organ transplants[1].
(E)-Methyl 3,4,5-trimethoxycinnamate is a bioactive natural phenylpropanoid. (E)-Methyl 3,4,5-trimethoxycinnamate suppresses inflammation in RAW264.7 macrophages and blocks macrophage-adipocyte interaction. (E)-Methyl 3,4,5-trimethoxycinnamate also has antiarrhythmic effect, leads to suppression of triggered activities in rabbit myocytes[1][2].
Chymase-IN-1 is a potent, selective, orally active, nonpeptide inhibitor of human mast cell chymase with an IC50 of 29 nM.
(S)-Lisofylline ((S)-Lisophylline)) is a kind of lisofline (LSF) enantiomer with optical activity. (S)-Lisofylline can interconversion with pentoxifylline[1][2].
Chebulagic acid is a COX-LOX dual inhibitor isolated from the fruits of Terminalia chebula Retz, on angiogenesis.target: COX-LOX [1]In vitro: Chebulagic acid can enhance the autophagy. Chebulagic acid exert anti-inflammatory and anti-infective effects. [1] [2] Chebulagic acid also show a protective effect against 1-methyl-4-phenylpyridinium (MPP+) - induce cytotoxicity which mimics the pathological symptom of Parkinson's disease. Chebulagic acid inhibit the LPS-induced upregulation of TNF-α and IL-1β in a dose- and time-dependent manner. Furthermore, LPS-activated MAPK signaling is inhibited by CA treatment in the EA.hy926 cells. [3]
ACT-777991 is an orally active and selective CXCR3 antagonist. ACT-777991 has microsomes and hepatocytes stability across animal models. ACT-777991 inhibits the migration of activated T cells toward CXCL11[1].
PA-9 is a pituitary adenylate cyclase-activating polypeptide (PACAP) type I (PAC1) receptor antagonist. PA-9 dose dependently inhibits PACAP-induced cAMP elevation with an IC50 of 5.6 nM. PA-9 can be used for the research of neuropathic and/or inflammatory pain[1].
Chloroquine dihydrochloride is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine dihydrochloride is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine dihydrochloride is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
Kadsurenin B is a PAF (platelet-activating factor) antagonist with neuroprotective activity. Kadsurenin B has a wide range of pharmacological research potential, such as antibacterial, anti-inflammatory, neuroprotective, antioxidant, antiplatelet aggregation, cytotoxic, antiparasitic, etc[1][2].
CL2A is a complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. Labetuzumab govitecan used this linker[1].
Ravagalimab (ABBV-323) is a CD40 antagonist (EC50: 3.7 nM). Ravagalimab can be used for research of Crohn's disease[1].
Bimosiamose is a pan-selectin antagonist, inhibits E-, P-, and L-selectin with IC50s of 88 μM, 20 μM, and 86 μM, respectively, and can be used in the research of inflammatory disease.
Hibifolin, a flavonol glycoside, is a potential inhibitor of adenosine deaminase (ADA), with a Ki of 49.92 μM. Hibifolin protects neurons against beta-amyloid-induced neurotoxicity[1][2].
WKYMVM is a potent N-formyl peptide receptor (FPR1) and FPRL1/2 agonist, also activates several leukocyte effector functions such as chemotaxis, mobilization of complement receptor-3, and activation of the NADPH oxidase[1][2].
Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties[1][2][3].
AS2521780 is a novel PKCθ selective inhibitor with an IC50 of 0.48 nM.
Tetomilast (OPC-6535) is a PDE4 inhibitor with potential for the treatment of inflammatory bowel disease (IBD) and chronic obstructive pulmonary disease (COPD).
Valategrast (R-411 free base) is a potent and orally active integrin α4β1 (VLA-4) and α4β7 dual antagonist. Valategrast has the potential for Chronic obstructive pulmonary disease (COPD) and asthma treatment[1][2].