Hypoletin-7-O-β-D-xylopyranoside is a natural compound with antioxidant activity[1].
bpV(phen) trihydrate, a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) trihydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) trihydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) trihydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity[1][2][3][4][5].
Strictosamide has important effects on inflammation and inflammatory pain. Strictosamide possesses antiplasmodial and antifungal activities[1].
Levocabastine (R 50547) hydrochloride is a long acting, highly potent and selective histamine H1-receptor antagonist with anti-allergic activity. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2[1][2].
sEH inhibitor-7 (compound c-2) is an inhibitor of soluble epoxide hydrolase (sEH) with IC50s of 0.15 μM (mouse sEH) and 6.2 μM (human sEH), respectively. soluble epoxide hydrolase (sEH) plays an important role in the metabolism of endogenous chemical mediators involved in the regulation of blood pressure and inflammation[1].
11-Hydroxytephrosin is a potent inhibitor of NF-kappaB. NF-kappaB is known to play a crucial role in the regulation of genes controlling the immune system, apoptosis, tumor cell growth, and tissue differentiation[1].
trans-β-terpineol, a monoterpenoid compound, can be isolated from the leaves of Schinus terebinthifolius. Terpineol has antioxidant and antibacterial activity. trans-β-terpineol is a bioactive compound that plays an antibacterial role in Schinus terebinthifolius[1].
MRS5698 is a selective Gi protein-coupled A3 adenosine receptor (A3AR) agonist, with Kis of approximately 3 nM for human and mouse A3AR, respectively. MRS5698 can be used for the research of pain and psoriasis[1][2].
4-Methoxylonchocarpin is an orally active anti-inflammatory agent. 4-methoxylonchocarpin inhibits the binding of LPS to Toll-like Receptor (TLR) TLR4 to inhibit NF-κB activation and TNF Receptor and IL-6 expression. 4-Methoxylonchocarpin also inhibits the phosphorylation of TGF-beta activated kinase 1 and TNBS-induced expression of IL-1β, IL-17A, and TNF. 4-methoxylonchocarpin can improve 2,4, 6-trinitrobenzene sulfonic acid (TNBS)-induced colitis mouse model[1].
Vasicinolone, a natural alkaloid, exhibits anti-inflammatory and antimicrobial properties[1].
1-Hydroxy-2-methylanthraquinone exhibits antimicrobial, antioxidant, pesticidal, and anti-inflammatory activities[1].
VPC23019, an aryl amide-containing Sphingosine 1-phosphate (S1P) analog, is a competitive antagonist at the S1P1 and S1P3 receptors (pKi= 7.86 and 5.93, respectively) and a agonist at the S1P4 and S1P5 receptors (pEC50= 6.58 and 7.07, respectively)[1].
AM095 is a selective LPA1 receptor antagonist. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively.
NLRP3-IN-25 (compound 32) is an orally available NLRP3 inhibitor with anti-inflammatory activity. NLRP3-IN-25 attenuates renal injury in doxorubicin-induced glomerulonephritis in mice. NLRP3-IN-25 inhibits IL-1β secretion in THP-1 cells with an IC50 of 21 nM[1].
IL-17 modulator 4 sulfate is a prodrug of IL-17 modulator 1 (HY-141535). IL-17 modulator 1 is an orally active, highly efficacious IL-17 modulator[1].
α,β-Methylene ATP dilithium, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand[1]. α,β-Methylene ATP dilithium is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7[2].
γ-Tocotrienol is an active form of vitamin E[1].
Melrilimab (GSK 3772847) is an IgG2-kappa anti-IL1RL1/ST2/IL33R/DER4/FIT-1 monoclonal antibody. Melrilimab can be used for the research of asthma[1].
Dapsone hydroxylamine (DDS-NOH) induces methemoglobinemia. Dapsone hydroxylamine inhibits catalase (CAT) activity and reactive oxygen species generation. Dapsone hydroxylamine also has anti-inflammatory activity[1].
(S)-(-)-Levamisole (Levamisole), an anthelmintic agent with immunomodulatory properties. (S)-(-)-Levamisole acts as a positive allosteric modulator (PAM) for the α3β2 (EC50=300 μM) and α3β4 (EC50=100 μM) subtype of nAChRs. Orally active[1][2].
Pyripyropene A is a potent and selective sterol O-acyltransferase 2 (SOAT2)/acyl-coenzyme A:cholesterol acyltransferase 2 (ACAT2) inhibitor, with an IC50 of 0.07 µM. Pyripyropene A attenuates hypercholesterolemia and atherosclerosis in vivo[1][2][3][4].
Chitoheptaose heptahydrochloride is a chitosan oligosaccharide with antioxidant, anti-inflammatory, antiapoptotic and cardioprotective activities. Chitoheptaose heptahydrochloride significantly enhances the growth and photosynthesis parameters of wheat seedlings[1][2].
PDE4-IN-9 (Compound 5j) is a potent inhibitor of PDE4. PDE4-IN-9 exhibits lower IC50 value (1.4 μM) against PDE4 than parent rolipram (2.0 μM) in in vitro enzyme assay. PDE4-IN-9 also displays good in vivo activity in animal models of asthma/COPD and sepsis induced by LPS[1].
Luffariellolide is an inhibitor of human synovial fluid phospholipase A2 (HSF-PLA2) (IC50=5 μM). Luffariellolide effectively inhibits phorbol ester (PMA)-induced ear edema (ED50=50 μg/ear)[1].
Izilendustat (hydrochloride) is a potent inhibitor of prolyl hydroxylase which stabilizes hypoxia inducible factor- 1 alpha (HIF- lα), as well as hypoxia inducible factor-2 (HIF-2). Izilendustat (hydrochloride) has the potential for the research of HIF- lα related diseases including Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, anemia, colitis, and other inflammatory bowel diseases (extracted from patent WO2011057115A1/WO2011057112A1/WO2011057121A1)[1][2][3].
Valeryl salicylate is a potent and irreversible cyclooxygenase-1 (COX-1) inhibitor. Valeryl salicylate shows anti-inflammatory effect[1].
FR122047 (hydrochloride) is a selective and oral active inhibitor of COX-1 with an IC50 of 28 nM. FR122047 hydrochloride has antiplatelet, analgesic and anti-inflammatory effects in vivo[1][2][3].
Lucidenic acid F, a natural triterpenoid, possesses anti-Inflammatory and anti-tumor activity[1].
Syk Inhibitor II dihydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride shows less potent against other kinases and has anti-allergic effect[1].
AGN194204 (IRX4204) is an orally active and selective RXR agonist with Kd values 0.4 nM, 3.6 nM and 3.8 nM and EC50s of 0.2 nM, 0.8 nM and 0.08 nM for RXRα, RXRβ and RXRγ, respectively. AGN194204 is inactive against RAR. AGN194204 has anti-inflammatory and anticarcinogenic actions[1][2].