L-Lysine-d4 is the deuterium labeled L-Lysine. L-lysine is an essential amino acid[1][2][3] with important roles in connective tissues and carnitine synthesis, energy production, growth in children, and maintenance of immu
Balicatib(AAE-581) is a potent and selective inhibitor of cathepsin K; 10-100 fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S.IC50 value:Target: cathepsin KThe cathepsin K inhibitor AAE-581 (balicatib) as the most advanced of them passed Phase II clinical trials in 2005. Eighty adult female Macaca fascicularis underwent bilateral ovariectomies and were dosed twice daily by oral gavage with balicatib at 0, 3, 10, and 50 mg/kg for 18 months (groups O, L, M, H, respectively). Approximately 1 month after treatment initiation, the 50 mg/kg dose was decreased to 30 mg/kg. Twenty animals underwent sham-ovariectomies (group S). Bone mass was measured at 3-6 month intervals. At 18 months, vertebra and femur were collected for histomorphometry.
Polyketide synthase 13-IN-2 (comp 42) is a polyketide synthase 13 inhibitor against Mycobacterium tuberculosis, with an MIC of 0.25 μg/mL[1].
ICI 162846 is an orally active antagonist of H2 receptor. ICI 162846 inhibits acid production accompanied by an increase in the secretion of histamine in chronic duodenal ulcer (CDU) models. ICI 162846 is effective in preventing CDU[1][2].
Z-LEHD-FMK TFA is an irreversible caspase-9 inhibitor, protects against lethal reperfusion injury and attenuate apoptosis[1][2].
LJP 1586 is an amine-based inhibitor of semicarbazide-sensitive amine oxidase (SSAO) activity. LJP 1586 is an orally active, potent and selective inhibitor of rodent and human SSAO activity, with IC50 values between 4 and 43 nM[1].
Elasnin is a selective granulocyte elastase inhibitor. Elasnin is almost ineffective for pancreatic elastase, trypsin, chymotrypsin, thermolysin and papain[1].
Stapokibart (CM310) is a humanised monoclonal antibody targeting IL-4Rα and efficiently blocks the interaction of cytokines IL-4 and IL-13 with their co-receptor subunit IL-4Rα. Stapokibart has the capacity to interact with IL-4Rα in humans, cynomolgus monkeys, and rats[1].
PKC-theta inhibitor 1 is the PKCθ inhibitor with an Ki value of 6 nM, inhibits IL-2 production in vivo with an IC50 of 0.19 μM. PKC-theta inhibitor 1 demonstrates a reduction of symptoms in a mouse model of multiple sclerosis[1].
Emeramide is a novel lipid-soluble, thiol-redox antioxidant and heavy metal chelator.
RPT193 is an orally active inhibitor of CCR4, blocks the recruitment of Th2 inflammatory immune cells into inflamed tissues. RPT193 can be used for allergic inflammation in atopic dermatitis, asthma, and other diseases research[1].
Caerulomycin A (Cerulomycin; Caerulomycin), an antifungal compound, induces generation of T cells, enhances TGF-β-Smad3 protein signaling via suppressing interferon-γ-induced STAT1 signaling. Antifungal and antibiotic activity, and used in autoimmune diseases[1].
Sappanone A is a homoisoflavanone which exhibits anti-inflammatory effects via modulation of Nrf2 and NF-κB. Sappanone can attenuate allergic airway inflammation in Ovalbumin-induced asthma[1].
H4R antagonist 2 (page 68), a Furo[3,2-d]pyrimidine derivative, is a potent H4R antagonist. H4R antagonist 2 can be used in research of rheumatoid arthritis[1].
Niazinin is a thiocarbamate glycoside with antileishmanial activities, with an IC50 value of 5.25 μM. Niazinin also shows a binding affinity with the target protein 3CL protease. Niazinin has promising leishmanicidal, anti-inflammatory and anti-pyretic activity[1][2].
BTT-3033 is an orally active conformation-selective inhibitor of α2β1 (EC50: 130 nM) by binding to the α2I domain. BTT-3033 inhibits platelet binding to collagen Ⅰ and cell proliferation, and induces cell apoptosis. BTT-3033 can be used in the research of prostate cancer, inflammation and cardiovascular disease[1][2][4].
Bromfenac is a potent and orally active inhibitor of COX, with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac can be used in ocular inflammation research[1].
1,3,5,8-Tetrahydroxyxanthone (Desmethylbellidifolin) is a natural xanthone extracted from Gentianella acuta. 1,3,5,8-Tetrahydroxyxanthone has antispasmodic effect and anti-inflammatory activity[1].
Diffractaic acid, a major constituent of U. longissimi, acts as an effective proapoptotic agent in various disorders research[1]. Diffractaic acid is the analgesic and antipyretic component of Usnea diffracta[2].
Citric acid is a weak organic tricarboxylic acid found in citrus fruits. Citric acid is a natural preservative and food tartness enhancer.
Humantenmine, a newalkaloid isolated from Gelsemium elegan Banth in China, has the potential for pain and rheumatic arthritis treatment[1][2].
Diacerein, a interleukin-1 beta inhibitor, is a slow-acting medicine of the class anthraquinone used to treat joint diseases.Target: IL-1 betaDiacerein, a interleukin-1 beta inhibitor, is a slow-acting medicine of the class anthraquinone used to treat joint diseases. Diacerein works by blocking the actions of interleukin-1 beta, a protein involved in the inflammation and destruction of cartilage that play a role in the development of symptoms of degenerative joint diseases such as osteoarthritis. Due to its specific mode of action, which does not involve the inhibition of prostaglandin synthesis, diacerein has been shown to have anti-osteoarthritis and cartilage stimulating properties in vitro and animal models, together with analgesic and anti-inflammatory properties. Due to its excellent gastro-intestinal tolerance, a combination therapy with an analgesic or a NSAID may be recommended during the first 2-4 weeks of treatment. From Wikipedia.
Alicaforsen 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.
Ginsenoside Rg5 is the main component of Red ginseng. Ginsenoside blocks binding of IGF-1 to its receptor with an IC50 of ~90 nM. Ginsenoside Rg5 also inhibits the mRNA expression of COX-2 via suppression of the DNA binding activities of NF-κB p65.
PS-1145 (dihydrochloride) is a potent IκB kinase-2 inhibitor with an IC50 value of 88 nM. PS-1145 (dihydrochloride) inhibits activity of NF-κB by blocking IκB kinase phosphorylation in tumor-bearing rats[1].
Bromodomain inhibitor-12 edisylate (example 303) is a bromodomain inhibitor that can be used in the research of autoimmune and inflammatory diseases[1].
Orniplabin (SMTP-7) is a low-molecular-weight compound that enhances plasminogen–fibrin binding, urokinase-catalyzed activation of plasminogen, and urokinase and plasminogen-mediated fibrin degradation. Orniplabin shows potential thrombolytic and anti-inflammatory effects. Orniplabin inhibits ROS[1][2].
Guanosine 5'-diphosphate (GDP) sodium is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate sodium is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate sodium can be used in the research of inflammation, such as anemia of inflammation (AI)[1][2].
Vitamin E, an essential nutrient for humans and animals reproduction, is a lipid-soluble antioxidant. Vitamin E can protect lipids against oxidative stress, and rescue the glutathione (GSH) depletion-induced hypersensitivity of cells to H2O2. Supplementation with Vitamin E increases its levels in cerebrospinal fluid and plasma, as well as reduces Aβ levels, thus beneficially influences oxidative stress in Alzheimer's disease. Vitamin E also has anti-aging effects[1][2][3][4].
Aucuparin, a natural product found in Sorbus aucuparia, inhibits pulmonary fibrosis in a bleomycin (BLM)-induced lung fibrosis mouse model. Anti-inflammatory activity[1][2].