Firocoxib-d4 (ML 1785713-d4) is the deuterium labeled Firocoxib. Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects[1].
UK-52831, a calcium channel antagonist, is used potentially for the treatment of hypertension and myocardia ischemia.
Plasmin is an important protease present in blood that degrades many plasma proteins, including fibrin clots. Plasmin can also act as a potent regulator of the immune process and can directly interact with various cell types, including monocytes, macrophages, and dendritic cells[1][2].
Difenpiramide (Z-876) is a bisphenylalcanoic derivative with marked anti-inflammatory, analgesic, antipyretic and uricosuric properties. Difenpiramide has platelet anti-aggregation activity[1].
Pimprinine is a potent monoamine oxidase inhibitor, could be isolated from fermented broths. Pimprinine has antioxidative activity and anticonvulsant activity. Pimprinine inhibits tremorine-induced tremors and analgesia in mice[1][2][3].
Hapten Dca is an immunizing hapten. Hapten Dca is activated by a solution of N, N′-disuccinimidyl carbonate. Hapten Dca with a carboxyl functional group is conjugated to proteins[1].
Proglumetacin is an orally active and potent cyclo-oxygenase inhibitor. Proglumetacin can inhibits SARS-CoV Mpro (main protease of the SARS-CoV-2), with an AC50 of 8.9 μM (activity concentration at half maximal activity). Proglumetacin has anti-inflammatory activity, can be used for inflammation (such as Rheumatoid arthritis, and Allergic air pouch inflammation) research[1][2][3].
Nusinersen is an antisense oligonucleotide drug that modifies pre–messenger RNA splicing of the SMN2 gene and thus promotes increased production of full-length SMN protein[1].
Meloxicam is a non-steroidal antiinflammatory agent, inhibits COX activity, with IC50s of 0.49 µM and 36.6 µM for COX-2 and COX-1, respectively.
KY-556 is a promising and orally-active pro-drug of disodium cromoglycate (DSCG) against allergic diseases.
Novel potent and selective antagonist of human Complement C3a receptor
8-O-Acetylharpagide is an iridoid isolated from Ajuga reptans with antitumoral, antiviral, antibacterial, and anti-inflammatory activities. 8-O-Acetylharpagide also has a biological activity on isolated smooth muscle preparations from guinea pig[1][2].
Peimine(Dihydroisoimperialine; Verticine) is a natural compound with good anti-inflammatory effects in vivo.IC50 value:Target:Peimine (0-25 mg/L) significantly inhibited tumor necrosis factor (TNF)-α, interleukin (IL)-6, IL-1β, and increased IL-10 production. Furthermore, peimine significantly inhibited the phosphorylation of p38, ERK and c-jun N-terminal kinase (JNK) as well as decreased p65 and IκB.
Reproxalap (ADX-102) is a reactive aldehyde species (RASP) sequestering agent for the treatment of dry eye. Reproxalap (ADX-102) covalently binds aldehydes including malondialdehyde and 4-hydroxynonenal[1][2].
LY306669 is a potent and selective leukotriene B4 (LTB4) receptor antagonist that can be used for the research of lung injury[1].
C25-140, a first-in-class TRAF6-Ubc13 inhibitor, directly binds to TRAF6, thereby blocks the interaction of TRAF6 with Ubc13 and as a consequence lowers TRAF6 activity. C25-140 expands studying the impact of the ubiquitin system on immune signaling and underscores the importance of TRAF6 E3 ligase activity in psoriasis and rheumatoid arthritis (RA)[1].
Sirtuin modulator 5 is a sirtuin modulating agent. Sirtuin modulator 5 can activate SIRT1 with a DC50 value of <50 μM. Sirtuin modulator 5 can be used for increasing the lifespan of a cell and used for the research of variety of diseases including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benfit from increased mitochondrial activity[1].
Aclidinium Bromide(LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist as a maintenance treatment for chronic obstructive pulmonary disease (COPD). IC50 value:Target: M3 receptorPreclinically, aclidinium showed potent antagonism of human muscarinic receptors, with a long residence time at M3 receptors and a shorter residence time at M2 receptors, indicating the potential to provide sustained bronchodilation. Aclidinium is rapidly hydrolysed in human plasma, unlike other currently available antimuscarinics including tiotropium. Early clinical studies in healthy subjects have confirmed the low systemic bioavailability and favourable safety profile of single and multiple doses of aclidinium. In a subsequent Phase IIb study, which included 464 patients with moderate to severe COPD, aclidinium displayed long-lasting bronchodilatory activity and was well tolerated.
PythiDC is a selective collagen prolyl 4-hydroxylase (CP4H1) inhibitor with an IC50 value of 4.0 μM. PythiDC can be used as a CP4H probe and also can be used for the development of a new class of antifibrotic and antimetastatic agents[1].
Acanthoside B is a potential bioactive lignan with anti-inflammatory and anti-amnesic activities. Acanthoside B can be used for alzheimer's disease and lung inflammation research[1]
Rocatinlimab (AMG 451) (KHK4083) is a fully human, non-fucosylated, immunoglobulin G1 (IgG1) anti-OX40 monoclonal antibody. Rocatinlimab can be used for the research of atopic dermatitis (AD)[1].
Roflumilast N-oxide is a PDE type 4 inhibitor.
Heparan sulfate, a complex and linear polysaccharide, exists as part of glycoproteins named heparan sulfate proteoglycans, which are expressed abundantly on the cell surface and in the extracellular matrix.
HER2-IN-8 is a HER-2 inhibitor extracted from patent WO2021179274A1 compound 107. HER2-IN-8 can be used for the research of cancer and inflammation[1].
Gefapixant is an orally active P2X3 receptor (P2X3R) antagonist with IC 50s of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.
Alniditan (Alnitidan) dihydrochloride is a potent 5-HT1B and 5-HT1D receptors agonist, with IC50s of 1.7 nM and 1.3 nM for h5-HT1B and h5-HT1D receptors in HEK 293 cells, respectively. Alniditan dihydrochloride has migraine-preventive effects[1][2].
7-O-Demethyl rapamycin, a derivative rapamycin (HY-10219), has antifungal activity and also immunosuppressant properties. 7-O-Demethyl rapamycin has useful tumor cell growth-inhibiting activity[1].
LMP7-IN-2 is a LMP7 inhibitor. LMP7-IN-2 can be used for associated inflammatory diseases and disorders[1].
Dihomo-γ-Linolenic acid is an n-6 polyunsaturated fatty acid that is mainly metabolized to an anti-inflammatory eicosanoid, prostaglandin (PG) E1, via the cyclooxygenase (COX) pathway. Anti-inflammatory and anti-proliferative effects[1][2].
Feprazone (DA2370; Prenazone), an analogue of Phenylbutazone (HY-B0230), is a nonsteroidal anti-inflammatory agent with analgesic and antipyretic activities. Feprazone acts by inhibiting the activity of cyclooxygenase (COX)-2. Feprazone ameliorates free fatty acid (FFA)-induced oxidative stress by reducing the production of mitochondrial reactive oxygen species (ROS). Feprazone can decrease the expression of MMP-2 and MMP-9. Besides, Feprazone can suppress adipogenesis and increase lipolysis in differentiating 3 T3-L1 cells. Feprazone also can be used to research atherosclerosis and obesity[1][2][3].