Methylprednisolone aceponate (ZK 91588) is a glucocorticoid and anti-inflammatory agent with weak systemic effects. Methylprednisolone aceponate is a selective glucocorticoid receptor Ligand.Methylprednisolone aceponate can be used for research of eczema and other inflammatory skin disorders[1][2][3].
Pantoprazole-d3 is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI)[1]. Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142)[3][4].
Palmitoyl tripeptide-8 s a bioactive peptide with anti-allergen effect and has been reported used as a cosmetic ingredient[1].
Bracteatin is a natural product that can be isolated from Actinidia arguta. Bracteatin has antioxidant effect.[1].
Acloproxalap is a quinoline-based aldehyde scavenger that can be used in studies of diseases with toxic aldehyde accumulation, such as inflammatory diseases of the eye and skin, respiratory diseases such as pneumonia, organ diseases, and viral infection-related syndromes[1][2].
MOG peptide (79-96) rat is a myelin oligodendrocyte glycoprotein (MOG) with encephalitogenic effects[1].
(rel)-Atorvastatin, a relative configuration of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively[1][2][3].
PKUMDL-LC-101-D04 (GPX4-Activator-1d4) is a potent ferroptosis regulator glutathione peroxidase 4 (GPX4) allosteric activator (pEC50=4.7). PKUMDL-LC-101-D04 increases GPX4 activity to 150% at 20 μM in the cell-free assay and 61 μM in cell extracts[1].
IC 86621 is a potent DNA-dependent protein kinase (DNA-PK) inhibitor, with an IC50 of 120 nM. IC 86621 also acts as a selective and reversible ATP-competitive inhibitor.IC 86621 inhibits DNA-PK mediated cellular DNA double-strand break (DSB) repair (EC50=68 µM). IC 86621 increases DSB-induced antitumor activity without cytotoxic effects. IC 86621 can protects rheumatoid arthritis (RA) T cells from apoptosis[1][2].
Picroside IV is an iridoid glycoside found in the underground parts of Picrorhiza scrophulariiflora. Picroside IV is a derivative of Catalpol (HY-N0820)[1]. Catalpol has neuroprotective, hypoglycemic, anti-inflammatory, anti-cancer, anti-spasmodic, anti-oxidant effects and anti-HBV effects[2].
Hedragonic acid is an oleane-type triterpenoid compound, which can be isolated from the stems and roots of the southern snake vine. Hedragonic acid is a ligand and agonist for FXR. Hedragonic acid protected mice from liver damage caused by acetaminophen overdose and reduced liver inflammation[1].
Vinaginsenoside R3 is a saponin composition of roots of Panax ginseng. Ginsengs have been not only used as therapeutic agents with tonic, sedative, anti-fatigue, and anti-gastric ulcer effect but also marketed as dietary supplements and raw materials of health food[1].
Tenoxicam, an antiinflammatory agent with analgesic and antipyretic properties.Target: COXTenoxicam is a non-steroidal anti-inflammatory drug (NSAID). Tenoxicam-treated patients had significant decrease in nitrite levels (p = 0.036) and XO activity (p = 0.01), but their SOD, GSH-Px enzyme activities, and MDA levels were unchanged from baseline. Tenoxicam may have antioxidant effects, and it may reduce nitrite levels, indicating an alteration of NO pathways [1]. Tenoxicam was administered intraperitoneally immediately after BCAO. Histological analyses show that ischemia produced significant striatal as well as hippocampal lesions which were reversed by the Tenoxicam treatment. Tenoxicam also significantly reduced, to control levels, the increased myeloperoxidase activity in hippocampus homogenates observed after ischemia [2].
Anhydroglycinol is a phenolic compound that can be isolated from Lespedeza homoloba. Anhydroglycinol has strong antioxidative and antiallergic activity against lipid peroxidation in the rat[1].
Etavopivat is a potent, selective, orally bioavailable red blood cell (RBC) pyruvate kinase (PKR) activator. Etavopivat has potent antisickling effects[1].
Albiflorin is a major constituent contained in peony root; possesses therapeutic potential for neurodegenerative diseases.IC50 value:Target: in vitro: Albiflorin significantly ameliorated Glu-induced reduction of cell viability, nuclear and mitochondrial apoptotic alteration, reactive oxygen species accumulation, and B-cell lymphoma 2 (Bcl-2)/Bax ratio. Albiflorin also enhanced phosphorylation of AKT and its downstream element glycogen synthase kinase-3β, and this effect was abrogated by the AKT inhibitor LY294002 [1]. in vivo: Mice were exposed to X-ray radiation (400 Roentgen), and both mice and rabbits were intraperitoneally injected with cyclophosphamide (100.0 mg/kg) and cytarabine chloride (92.7 mg/kg), respectively, for 3 days to induce myelosuppression. Albiflorin was subsequently administrated intravenously at low (15.0 mg/kg for mice, 6.00 mg/kg for rabbits), intermediate (30.0 mg/kg for mice, 12.0 mg/kg for rabbits) and high (60.0 mg/kg for mice, 24.0 mg/kg for rabbits) doses, as well as orally (60.0 mg/kg for mice, 24.0 mg/kg for rabbits) for 7 days. Shenqi tablets were used as positive controls (oral administration of 936.0 mg/kg for mice, 336.0 mg/kg for rabbits). The administration of Albiflorin significantly ameliorated myelosuppression in all cases [2].
IKK 16 hydrochloride is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively[1]. IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC50 of 50 nM[2].
Alicaforsen sodium?is a 20-base antisense oligonucleotide inhibiting ICAM-1 production, which is an important adhesion molecule involved in leukocyte migration and trafficking to the site of inflammation.
Levocabastine (R 50547) is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC)[1][2][3].
HIF-2α-IN-7 is a hypoxia inducible factor 2α (HIF-2α) inhibitor. HIF-2α-IN-7 can inhibit HIF-2α with an EC50 value of 6nM. HIF-2α-IN-7 can be used for the research of various types of diseases including cancer, liver disease, inflammatory disease, pulmonary diseases and iron load disorders[1].
Kaurenoic acid is a diterpene from Sphagneticola trilobata, inhibits Inflammatory Pain by the inhibition of cytokine production and activation of the NO–cyclic GMP–PKG–ATP-sensitive potassium channel signaling pathway[1].
Scoparinol (Scopadiol) is a diterpene isolated from Scoparia dulcis that has significant analgesic and anti-inflammatory activities[1].
Tegomil fumarate is an immunomodulator[1].
P2X3 antagonist 38 (compound 4) is a potent and orally active P2X3 antagonist with IC50 values of 0.132, 0.165, 0.421 µM for hP2X3, rP2X3, gpP2X3, respectively[1].
Alpinetin is a flavonoid isolated from Alpinia katsumadai Hayata, activates activates PPAR-γ, with potent anti-inflammatory activity[1].
Chelerythrine Chloride is a potent, cell-permeable inhibitor of protein kinase C, with an IC50 of 660 nM.
iNOS-IN-2 (Compound 53) is a potent down-regulator of inducible nitric oxide synthase (iNOS) protein. iNOS-IN-2 effectively inhibits the NO production (IC50=6.4 μM). iNOS-IN-2 has a potential therapeutic effect on chronic inflammation[1].
GW311616 is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM; free base form of GW311616A.IC50 value: 22 nM [1]Target: neutrophil elastaseThe HNE inhibitor GW311616A is selective over other human serine proteases (IC50 values >100 uM for trypsin, cathepsin G, and plasmin, >3 mM for chymotrypsin and tissue plasminogen activator). Acetylcholinesterase is not inhibited by GW311616A at 100 uM.GW311616A is more potent than thetrifluoromethylketone inhibitor ZD8321 (Ki=13 nM). GW311616A is orallybioavailable in rat, dog (Table 4) and hamster despite moderate to high plasmaclearance, which indicates that clearance is predominantly extrahepatic.
RGX-104 is a small-molecule LXR agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The Ki values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells[1][2].