Benralizumab (MEDI-563) is an interleukin-5 receptor α (IL-5Rα)-directed cytolytic monoclonal antibody that induces direct, rapid and nearly complete depletion of eosinophils via enhanced antibody-dependent cell-mediated cytotoxicity. Benralizumab can be used to treat severe eosinophilic asthma[1].
HAMI3379 (HAMI-3379) is a potent and selective antagonist of cysteinyl leukotriene 2 (CysLT(2)) receptor, inhibits LTD4- and LTC4-induced intracellular calcium mobilization withIC50 of 3.8 nM and 4.4 nM respectively; exhibits very low potency on a recombinant CysLT(1) receptors (IC50>10 uM), does not exhibit any agonistic activity on both CysLT receptors; concentration-dependently inhibits and reverses the LTC(4)-induced perfusion pressure increase and contractility decrease in isolated Langendorff-perfused guinea pig hearts, protects against acute brain injury after focal cerebral ischemia in rats.
BN201 promotes neuronal differentiation, the differentiation of precursor cells to mature oligodendrocytes (EC50 of 6.3 μM) in vitro, and the myelination of new axons (EC50 of 16.6 μM). BN201 is able to cross the blood-brain barrier by active transport and activate pathways (IGF-1 pathway) associated with the response to stress and neuron survival. BN201 has potently neuroprotective effects[1].
Sotatercept (ACE-011) is a soluble activin receptor 2A (ACVR2A) type IgG Fc fusion protein. Sotatercept combines activin and growth differentiation factor to try to restore the balance between growth promotion and growth inhibition signal pathways. Sotatercept has potential application in pulmonary arterial hypertension, anemia, bone loss, erythropoiesis, multiple myeloma (MM) osteolytic lesions[1][2][3][4][5].
Ianthelliformisamine B diTFA is a bromotyrosine-derived antibacterial agent. Ianthelliformisamine B diTFA is against E. coli and S. aureus strains with MICs of 14.5 μM and 144.7 μM[1].
Z-Asp-CH2-DCB is an irreversible broad spectrum caspase inhibitor. Z-Asp-CH2-DCB also inhibits proteases with caspase-like activity. Z-D-CH2-DCB blocks the production of IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B (SEB)-stimulated peripheral blood mononuclear cells (PBMC), and reduces SEB-1-stimulated T-cell proliferation in a dose-dependent manner. Z-Asp-CH2-DCB prevents SU5416-induced septal cell apoptosis and emphysema development[1][2][3].
Benzoylalbiflorin is a monoterpenoid, and is isolated from Radix Paeoniae Alba. Radix Paeoniae Alba is a traditional Chinese medicine that has been used for the research of rheumatoid arthritis, to alleviate inflammation, amenorrhea, epistaxis, abdominal pain, and other symptoms[1].
Osajin is the major bioactive isoflavone present in the fruit of Maclura pomifera with antitumor, antioxidant and anti-inflammatory activities.
STAT6-IN-1 (compound 19a) is a STAT6 inhibitor with a high affinity for the SH2 domain of STAT6 (IC50=0.028 µM). STAT6-IN-1 can be used in studies of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease or cancer[1][2].
Izuralimab is a bispecific IgG1 antibody targeting inducible T-cell costimulator (ICOS/CD278) and PD-1[1].
Schisantherin A is a dibenzocyclooctadiene lignan isolated from the fruit of Schisandra sphenanthera. Schisantherin A inhibits p65-NF-κB translocation into the nucleus by IκBα degradation.
TLK117, the active metabolite of TLK199, selective inhibits Glutathione S-transferase P1–1 (GSTP1-1) with a Ki of 0.4 μM for GSTP. TLK117 also competitively inhibits glyoxalase I with a Ki of 0.56 μM.
Aderamastat (FP-025) is an orally active matrix metalloproteinase 12 (MMP-12) inhibitor. Aderamastat can be used for the research of asthma, chronic obstructive pulmonary disease (COPD), and pulmonary fibrosis[1].
9α,11β-Prostaglandin F2α is an endogenous metabolite present in Urine that can be used for the research of Asthma[1][2].
ABT-102 is a potent and highly selective Vanilloid Receptor (TRPV1) receptor antagonist. ABT-102 potently and reversibly increases heat pain thresholds and reduced painfulness of suprathreshold oral/cutaneous heat. ABT-102 reduces nociceptive responses of animals in models of inflammatory, bone cancer, postoperative, and osteoarthritic pain[1][2].
MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 blocks Th17 cell differentiation and ameliorates colitis in mice[1].
UCB-6876 is a novel inhibitor of TNF signalling by stabilising an asymmetric form of the trimer, displaying a concentration-dependent response curve and selectivity over the TNFR1 extracellular domain and control proteins.
Pelargonidin 3,5-diglucoside (chloride) is a natural pigment abundantly present in red fruits and vegetables. Pelargonidin 3,5-diglucoside (chloride) acts as a scavenger for reactive oxygen species and reactive nitrogen species . Pelargonidin 3,5-diglucoside (chloride) demonstrates inhibitory effects on enzymes involved in the production of ROS, RNS, and pro-inflammatory cytokines[1].
Sudoxicam is a reversible and orally active COX antagonist and a non-steroidal anti-inflammatory drug (NSAID) from the enol-carboxamide class. Sudoxicam has potent anti-inflammatory, anti-edema and antipyretic activity[1][2][3].
AQX-435 is a potent SHIP1 activator. AQX-435 reduces PI3K activation downstream of the B-cell receptor (BCR) and induces apoptosis of malignant B cells, and reduces lymphoma growth[1].
Isoengeletin is a flavonoid that can be isolated from the roots of Smilax bockii warb. Isoengeletin can be used as an active compound for the research of psoriasis, hyperuricemia and gout[1].
Isoetharine (Isoetarine) mesylate is an orally active selective agonist of β-adrenergic receptors. Isoetharine mesylate is a catechol-like drug and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine mesylate can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator[1][2].
Lys-Gln-Ala-Gly-Asp-Val (KQAGDV) is the six most carboxyl-terminal amino acids in the fibrinogen γ-chain sequence. Lys-Gln-Ala-Gly-Asp-Val is a cell adhesion peptide which is mediated through the α2bβ3 integrin. Lys-Gln-Ala-Gly-Asp-Val is a potent adhesion ligand for smooth muscle cells (SMCs)[1][2].
Ligelizumab (QGE 031) is a humanized high-affinity monoclonal anti-IgE antibody. Ligelizumab can be used for the research of chronic spontaneous urticarial[1].
TMP778 is a potent and selevtive RORγt inverse agonist, with an IC50 of 7 nM in FRET assay.
Alcindoromycin is an anthracycline antitumor antibiotic[1].
p38α inhibitor 1 is a p38α inhibitor extracted from patent WO 2008076265 A1.
Vonifimod is an immunomodulator[1].
RIPK1-IN-13 (Compound 8) is a potent inhibitor of RIPK1 with an IC50 value of 1139 nM. RIPK1-IN-13 blocks the activation of the necroptosis pathway via the inhibition of RIPK1. RIPK1-IN-13 has the potential for the research of inflammation diseases[1].
Octreotide is a somatostatin analog that binds to the somatostatin receptor, mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production.