RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pKi=9.04)[1].
Amphotericin B trihydrate, a polyene antibiotic, is first isolated from fermenter cultures of Streptomyces nodosus. Amphotericin B trihydrate also possesses antileishmanial activity[1][2].
Bucillamine (SA96) is an orally active and potent sulfhydryl donor and antioxidant. Bucillamine is also an antirheumatic agent with antiangiogenic properties. Bucillamine can protect against Ischemia/reperfusion (I/R) injury in high-risk organ transplants. Bucillamine inhibits the production of VEGF. Bucillamine can be used for the research of choroidal neovascularization (CNV) and rheumatoid arthritis (RA)[1][2].
P2Y2R/GPR17 antagonist 1 (Compound 14m) is a dual P2Y2R and GPR17 antagonist with IC50 values of 3.17 µM and 1.67 µM against P2Y2R and GPR17, respectively. P2Y2R/GPR17 antagonist 1 shows excellent metabolic stability in human liver microsomes[1].
XVA143, an α/β I-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo[1].
Piperlactam S is an active compound. Piperlactam S can be isolated from Piper kadsura. Piperlactam S can be used for the research of chronic inflammation[1].
Glucocorticoids receptor agonist 1 is a potent anti-inflammatory, arylpyrazole-based glucocorticoid receptor agonist that does not impair insulin secretion.
ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 230 nM for human NAAA. ARN19702 has pain relief effects[1][2].
Neuroinflammatory-IN-1 (Compound 5) is an anti-neuroinflammatory agent and displays inhibitory effect on nitric oxide (NO) production with an IC50 value of 65.4 μM[1].
NR2F6 modulator-1 is a potent nuclear receptor subfamily 2, group F, member 6 (NR2F6) modulator. NR2F6 modulator-1 can be used for researching immune modulation and modulation of cancer stem cell activity[1].
BTK-IN-27 (example 8) is a BTK inhibitor (IC50: 0.2 nM). BTK-IN-27 shows anti-proliferative activity in TMD8 cells (IC50: < 5 nM). BTK-IN-27 can be used for research of cancer, lymphoma, leukemia and immunological diseases[1].
Aquilarone C is a chromone derivative with anti-inflammatoryeffects[1].
Cynarin is an antichoke agent with a variety of biological activities including antioxidant, antihistamic and antiviral activities.
N-Acetyl-Ser-Asp-Lys-Pro is a natural and specific substrate for the N-terminal site of ACE.
MC-4R Agonist 2 (Example 1) is a MC4R agonist. MC-4R Agonist 2 can be used in the study of obesity, diabetes, inflammation, and erectile dysfunction[1].
PAR-4 Agonist Peptide, amide TFA (PAR-4-AP TFA; AY-NH2 TFA) is a proteinase-activated receptor-4 (PAR-4) agonist, which has no effect on either PAR-1 or PAR-2 and whose effects are blocked by a PAR-4 antagonist[1].
SHR0302 is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of SHR0302 for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. SHR0302 inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. SHR0302 has anti-proliferative and anti-inflammatory effects[1][2].
Prifelone (R 830; R 830T; S 16820) is a di-tert-butylphenol with anti-inflammatory and antioxidant activity. Prifelone inhibits guinea pig lung oxygenase and bovine seminal vesicle cyclooxygenase[1].
Baicalein 7-O-β-D-ethylglucuronide is a natural flavone glycoside that can be extracted from Scutellaria baicalensis Georgi. Baicalein 7-O-β-D-ethylglucuronide has antioxidant activity. Baicalein 7-O-β-D-ethylglucuronide inhibits FeSO4-Cys-induced lipid peroxidation of liver homogenate. Baicalein 7-O-β-D-ethylglucuronide also shows strong cytoprotective effect on H2O2-induced oxidative damage of human umbilical vein endothelial cells[1][2].
Osilodrostat (LCI699) is a potent inhibitor of human 11β-hydroxylase and aldosterone synthase with IC50 values of 2.5 and 0.7 nM, respectively.
CB2R/FAAH modulator-3 (compound 27) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-3 are 20.1 and 67.6 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 3.4 μM. CB2R/FAAH modulator-3 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection[1].
P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC50s of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect[1].
Chrysophanol tetraglucoside possesses anti-hypolipidemic and antibacterial activities[1][2].
Cerebroside D, a glycoceramide compound, improves experimental colitis in mice with multiple targets against activated T lymphocytes[1].
NFAT Transcription Factor Regulator is an IL-2 synthesis inhibitor with an IC50 of 182 nM.
Dropropizine is a racemic non-opiate antitussive agent which has been used clinically for many years.
Cepharadione A can be isolated from the roots of Piper betle Linn. Cepharadione A inhibits FMLP/CB induced elastase release by human neutrophils[1].
Baicalin is a flavonoid glycoside isolated from Scutellaria baicalensis. Baicalin reduces the expression of NF-κB.
Cyclic ADP-ribose (cADPR) is a potent second messenger for calcium mobilization that is synthesized from NAD+ by a ADP-ribosyl cyclase. Cyclic ADP-ribose increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels[1].