Coumarin 6H, a Coumarin (Coumarin (HY-N0709)) derivative, is a laser dye. The fluorescence emission of Coumarin 6H can be enhanced by hydrogen bonding interactions[1][2].
Triptohypol C, a Tripterin (HY-13067) derivative, is a potent Nur77-targeting anti-inflammatory agent with an Kd value of 0.87 μM. Triptohypol C inhibits inflammatory response by promoting the interactions of Nur77 with TRAF2 and p62/SQSTM1[1].
PBP10 is a cell permeable and selective gelsolin-derived peptide inhibitor of formyl peptide receptor 2 (FPR2) over FPR1[1]. PBP10 is a 10-AA peptide with rhodamine conjugated at its N terminus, exerts bactericidal activity against gram-positive and gram-negative bacteria and limits microbial-induced inflammatory effects[2].
Chrysophanol 8-O-β-D-(6’-O-galloyl)glucopyranoside, an anthraquinone glucoside, can be isolated from Rheum undulatum L. Chrysophanol 8-O-β-D-(6’-O-galloyl)glucopyranoside has potent DPPH radical and ?O2- scavenging activity[1].
Ramifenazone-d7 (Isopropylaminoantipyrine-d7) is the deuterium labeled Ramifenazone. Ramifenazone (Isopropylaminoantipyrine) is a pyrazole derivative and acts as a non-steroidal anti-inflammatory agent (NSAID). Ramifenazone has analgesic, antipyretic, anti-inflammatory and antimicrobial activities[1][2].
Contezolid acefosamil sodium (MRX-4), a new and orally active oxazolidinone, is an antibiotic in study for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. Contezolid acefosamil sodium (MRX-4) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI)[1][2].
Herpotrichone A shows potent anti-neuroinflammatory activity in lipopolysaccharide (LPS)-induced BV-2 microglial cells with the half maximal inhibitory concentration (IC50) value of 0.41 μM.
Danburstotug (IMC-001) is an IgG1-lambda anti-CD274 (PDL1, B7 homologue 1, B7H1) humanized monoclonal antibody. Danburstotug also is immunostimulant and antineoplastic[1].
(-)-Ibuprofenamide is an amide prodrug of Ibuprofen with anti-inflammatory activity[1]. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively[2].
Morusinol is a flavonoid isolated from Morus alba root bark. Morusinol has an antiplatelet activity and significantly inhibits arterial thrombosis in vivo[1].
Anisodamine hydrochloride is an anticholinergic and α1 adrenergic receptor antagonist. Anisodamine hydrochloride can be used for improving blood flow in circulatory disorders such as septic shock, Anisodamine hydrochloride displays a spectrum of pharmacological effects similar to Atropine (HY-B1205) and Sopolamine (HY-B2065) including inhibition of salivation, gastrointestinal and sweat secretion, gastrointestinal motility, respiratory secretion and urinary bladder contraction in vivo[1].
PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma.
COX-2-IN-36 (compound 1) is a very potent and specific COX-2 inhibitor, with an IC50 of 0.4 μM[1][2].
D18024 is a phthalazinonderivat antiallergic and antihistaminic activity.
ML261 is a hepatic lipid droplets formation inhibitor with an IC50 value of 69.7 nM. ML261 can be used for the research of non-alcoholic fatty liver disease (NAFLD) and inflammation[1].
IL-17A inhibitor 1 (example 24) is a IL-17A inhibitor, with IC50 values of <9.45 nM and 9.3 nM in alphalisa assay and HT-29 cells[1].
GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.IC50 value: 3.2 pM [1]Target: PDE4Bin vitro: GSK256066 is a slow and tight binding inhibitor of PDE4B with apparent IC50 of 3.2 pM. GSK256066 is an extremely potent inhibitor of LPS-stimulated TNFα production in PBMCs with pIC50 of 11.0 and IC50 of 10 pM and human whole-blood cultures with pIC50 of 9.90 and IC50 of 126 pM. GSK256066 is highly selective for PDE4 (>3.8 × 105-fold versus PDE1, PDE2, PDE3, PDE5, and PDE6 and >2.5 × 103-fold against PDE7). GSK256066 inhibits PDE4 isoforms A-D with equal affinity [1].in vivo: GSK256066 inhibits the LPS-induced pulmonary neutrophilia with an ED50 of 1.1 μg/kg, achieving maximal inhibition of 72% at 30 μg/kg when given in the aqueous suspension. GSK256066 inhibits the LPS-induced pulmonary neutrophilia with ED50 of 2.9 μg/kg, achieving maximal inhibition of 62% when given in the dry powder formulation. GSK256066 shows a moderate plasma clearance of 39 ml/min/kg, a moderate volume of distribution of 0.8 L/kg, and a relatively short half-life of 1.1 hour in the male CD rat [1]. GSK256066 sustains at a high lung concentration of 2.6 μg/g after intra-tracheal administration as an aqueous suspension at a dose of 30 μg/kg in rats [2]. GSK256066 (10 μg/kg) is administered intratracheally at different times (2, 6, 12, 18, 24, and 36 hours) before LPS administration, inhibiting LPS-Induced Pulmonary Neutrophilia in rat lipopolysaccharide (LPS)-induced models of acute pulmonary inflammation. GSK256066 (0.3–100 μg/kg) inhibits LPS-induced increases in exhaled nitric oxide with ED50 of 35 μg/kg in rat. GSK256066 (10 μg/kg) is administered half a hour before OVA administration in rat, inhibiting OVA-induced pulmonary eosinophilia with ED50 of 0.4 μg/kg. GSK256066 administered intratracheally as a dry powder blended in respiratory-grade lactose at doses of 3 to 100 μg/kg 2 hours before inhaled LPS challenge in ferrets, inhibiting LPS-induced pulmonary neutrophilia with ED50 of 18 μg/kg without inducing emetic episodes [3].
CFTR activator 1 is a potent and selective CFTR activator, with an EC50 of 23 nM. CFTR activator 1 can be used to ameliorate dry eye disease[1].
A-967079 is a selective TRPA1 receptor antagonist with IC50s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the CNS.
Buddlejasaponin IVb (Compound 2), a triterpene saponin isolated from Clinopodium chinense (Benth.) O. Kuntze, Compound 2 has hemostasis efficacy, shortens thrombin time (TT) by 20.6 %[1].
Gedunin is a limonoid with anti-cancer, anti-viral, anti-inflammatory and insecticidal activities. Gedunin acts as a potent Hsp90 inhibitor and induces the degradation of Hsp90-dependent client proteins. Geduni may obstructs the entry of SARS-CoV-2 virus into human host cells and can be used for COVID-19 research[3].
EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC50 values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEK cells). EDP-305 shows a potent and consistent antifibrotic effect. EDP-305 can be used for primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH) research[1][2].
S-Adenosyl-L-methionine D3 (S-Adenosyl methionine D3) is a deuterium labeled S-Adenosyl-L-methionine. S-Adenosyl-L-methionine is produced endogenously from methionine and ATP by action of the enzyme methionine adenosyltransferase and is an important orally active methyl group donor[1][2].
Tagitinin F is a sesquiterpene with potent anti-inflammatory properities and nuclear factor-kappa B inhibition. Tagitinin F inhibits ipopolysaccharide-induced myeloperoxidase activity in human neutrophils. Tagitinin F decreases the secretion of inflammatory products without inducing apoptosis in neutrophils[1].
MK-571 (L-660711) is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release[1][2][3].
Saccharin is an orally active, non-caloric artificial sweeteners (NAS). Saccharin has bacteriostatic and microbiome-modulating properties[1].
Morachalcone A is a naturally-occurring aromatase inhibitor (IC50=4.6 mM). Morachalcone A is also a plants metabolite with potential anti-inflammatory and anticancer activity. Morachalcone A inhibits Lipopolysaccharide (HY-D1056)-induced nitric oxide production[1][2][3].
GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC50=7.1)[1]. GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice[2][3].
Phenacetin is a non-opioid analgesic without anti-inflammatory properties, inhibits COX-3 activity.Target: COXPhenacetin is a pain-relieving and fever-reducing drug, Phenacetin was withdrawn from the Canadian market in June 1973 due to concerns regarding nephropathy. the clinical and laboratory data were compatible with "phenacetin nephritis" as described in Europe and Australia and recently in the United States and Canada. This report evaluates the findings in the 23 cases and cautions against the use of phenacetin, particularly in patients with impaired renal function [1]. Phenacetin has been linked to renal papillary necrosis in human beings [2, 3].
GW0742 is a high affinity PPAR β/δ agonist with an IC50 of 1 nM for human PPARδ, and EC50s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ, respectively.