Coenzyme Q0 (CoQ0) is a potent, oral active ubiquinone compound can be derived from Antrodia cinnamomea. Coenzyme Q0 induces apoptosis and autophagy, suppresses of HER-2/AKT/mTOR signaling to potentiate the apoptosis and autophagy mechanisms. Coenzyme Q0 regulates NFκB/AP-1 activation and enhances Nrf2 stabilization in attenuation of inflammation and redox imbalance. Coenzyme Q0 has anti-angiogenic activity through downregulation of MMP-9/NF-κB and upregulation of HO-1 signaling[1][2][3].
TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis[1][2].
Methylene blue (Basic Blue 9) hydrate is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue hydrate through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue hydrate is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue hydrate is a Tau aggregation inhibitor. Methylene blue hydrate reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation[1][2][3].
Sutimlimab, a first-in-class complement protein component 1, s subcomponent (C1s) inhibitor, can be used for the research of cold agglutinin disease. C1s is a serine protease which cleaves C4 and C2 to form the C3 convertase[1].
Mirococept (APT070) is an antibody targeting to complement system C3b/C4b, as well as a membrane-localizing C3 convertase inhibitor. Mirococept reduces the release of C-peptide and pro-inflammatory cytokines, and reduces the infiltration of inflammatory cells. Mirococept reduces intraislet inflammation, which is beneficial to islet transplantation. Mirococept also inhibits increased intestinal and pulmonary vascular permeability to reduce neutrophil influx[1][2].
diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist.
Lampalizumab (RG 7417) is a humanised monoclonal antibody targeting complement Factor D in the alternative complement pathway. Lampalizumab binds an exosite and sterically blocks Factor B access to the active site. Lampalizumab can be used for age-related macular degeneration (AMD) research[1][2].
Chlorcyclizine hydrochloride is a histamine H1 antagonist.
Salicylic acid inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation.
SKI-II is a synthetic inhibitor of sphingosine kinase (SK) activity with IC50 of 78 μM for SK1 and 45 μM for SK2.IC50 value: 78/45 μM (SK1/2) [2]Target: SKin vitro: SKI II inhibits cell proliferation by suppressing the Wnt/β-catenin signaling pathway. SKI II also reduces the expression of c-Myc and cyclin D1, the downstream target genes of the Wnt signaling pathway. SKI II inhibits cell proliferation by suppressing the Wnt/β-catenin signaling pathway. SKI II promotes the degradation of β-catenin by enhancing Wnt5A. SKI II inhibits the proliferation of HepG2 cells by blocking the Wnt/β-catenin signaling pathway. [1]in vivo: SKI-II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation. In the present study, SKI-II was administered 3-weekly i.p. to LDL-R-/- mice for 16 weeks at a dose previously demonstrated to reduce tumor growth in mice. Preliminary experiments revealed that a single administration of SKI-II produces a significant reduction of plasma S1P with the maximum (40%) observed 12 h after injection. [2]
Rupatadine D4 fumarate (UR-12592 D4 fumarate) is a deuterium labeled Rupatadine fumarate. Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 μM(rabbit platelet membranes/guinea pig cerebellum membranes)[1][2][3].
Famotidine is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.Target: Histamine H2 ReceptorFamotidine is a histamine H2-receptor antagonist that inhibits stomach acid production, and it is commonly used in the treatment of peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD/GORD). Famotidine Group(2 mg/kg/day) were significantly lower than the equivalent parameters for the Control Group on both the third and seventh days post-surgery. famotidine exerts detrimental effects on the anastomotic bursting pressure and hydroxyproline content of perianastomotic tissues in the colon of rats [1]. famotidine increased the transgastric potential difference (PD) and promoted the recovery of decreased transgastric PD induced by acidified ethanol in rats. The preventive effect of famotidine on gastric lesions is attributable not only to suppression of acid secretion but to activation of the gastric mucosal defensive mechanisms [2].
ODN 21158 is a potent G-modified TLR3 andTLR9inhibitor. ODN 21158 shows no cytotoxic. ODN 21158 nhibits IFN-α secretion in a dose dependent manner[1].
Indomethacin (Indometacin) sodium is a potent, orally active COX1/2 inhibitor with IC50 values of 18 nM and 26 nM for COX-1 and COX-2, respectively. Indomethacin sodium has anticancer activity and anti-infective activity. Indomethacin sodium can be used for cancer, inflammation and viral infection research.[1][2][3].
DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect[1][2].
diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist.
N,N-Dimethylsphingosine is a potent inhbitor of SphK (sphingosine kinase) as an endogenous metabolite of sphingosine produced in various tissues and tumor cell lines[1].
Mifepristone is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay.
TLR7 agonist 16 (compound 16d) is a highly potent TLR7 agonist with an EC50 of 18 nM. TLR7 agonist 16 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations[1].
Dexketoprofen trometamol (Dexketoprofen tromethamine salt) is an orally active non-selective COX inhibitor. Dexketoprofen trometamol has a pain-relieving effect[1].
Amaroswerin is a bioactive secoiridoid glucoside from Swertia mussotii. Amaroswerin has anti-inflammatory, antidiabetic, antiviral, anticholinergic and immunomodulatory activities. Amaroswerin inhibits NO release with an IC50 value of 5.42 μg/mL in RAW264.7 cells[1].
Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant (maleate) has the potential for attention-deficit hyperactivity disorder research[1][2][3][4].
Ebrotidine(FI 3542) is a competitive H2-receptor antagonist (Ki= 127.5 nM) with a potent antisecretory activity and evidenced gastroprotection.IC50 Value: 127.5 nM (Ki)[1]; 0.21mg/kg (ED50, histamine- stimulated acid secretion) [2]Target: H2 receptorin vitro: Ebrotidine displaced 3H-thiotidine specific binding to histamine H2-receptors (Ki: 127.5 nmol/l), showing a higher affinity (p < 0.05) than ranitidine (Ki: 190.0 nmol/l) and cimetidine (Ki: 246.1 nmol/l) [1]. in vivo: Following intravenous administration to rats, ebrotidine inhibited histamine- and pentagastrin-stimulated acid secretion in a dose-dependent manner, ED50 being 0.21 and 0.44 mg/kg, respectively [2]. The mean number of gastric erosions seen at endoscopy after treatment with ebrotidine plus ASA (2.0 +/- 0.3) was significantly lower than that after placebo plus ASA (3.7 +/- 0.2). This reduction in lesion core by ebrotidine was accompanied by a significant increase in gastric blood flow (by 15% in corpus and 26% in antrum), by a rise in transmucosal potential difference (by 12%), and by a decrease of mucosal microbleeding [3]. Results of macroscopic assessment revealed that ebrotidine at doses of 50mg and higher/kg body weight effectively prevented mucosal injury, and that the maximal protective effect was achieved by 1h. Physicochemical analysis established that ebrotidine evoked 30% increase in mucus gel dimension, and showed 20% increase in phospholipids, and the content of sulfo- (18%) and sialomucins (21%) [4].
Phenidone, an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), ameliorates rat paralysis in experimental autoimmune encephalomyelitis. Phenidone is a potent hypotensive agent in the spontaneously hypertensive rat[1][2]. Phenidone is used as a photographic developer[3].
Polyinosinic-polycytidylic acid sodium (Poly(I:C) sodium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis[1][2].
Cinnarizine is an antihistamine and a calcium channel blocker, promote cerebral blood flow, used to treat cerebral apoplexy, post-trauma cerebral symptoms, and cerebral arteriosclerosis.
Interleukin II (60-70) is a 60-70 fragment of the cytokine Interleukin II polypeptide[1].
Lipustobart is an IgG4-kappa, anti-PDCD1 (programmed cell death 1, PD1, PD-1, CD279) humanized monoclonal antibody. Lipustobart shows immunostimulant and antineoplastic activity[1].
L-NAME hydrochloride inhibits NOS with an IC50 of 70 μM. L-NAME is a precursor to NOS inhibitor L-NOARG which has an IC50 value of 1.4 μM.
Regaloside A, a phenylpropanoid, shows significant DPPH radical scavenging activity of 58.0% at 160 ppm. Regaloside A has anti-inflammatory activity[1].