Oliceridine (TRV130) is a novel mu opioid receptor (MOR) agonist that preferentially activates G-protein versus β-arrestin signaling pathways coupled to MORs.
Oleanolic aldehyde is an antimicrobial compound used to inhibit oral bacteria. Oleanolic aldehyde inhibits Streptococcus mutans and Porphyromonas gingivalis, which are associated with dental caries and periodontal disease, with minimum inhibitory concentrations (MICs) of 488 μg/mL and 250 μg/mL, respectively[1].
Thiophanat-ethyl-d10 is the deuterium labeled Thiophanat-ethyl[1].
Yadanzioside C is a quassinoid glucoside found in seeds of Brucea amarissima[1].
7-(Butyn-2-yl)-7,8-dihydro-8-oxo-9-(β-D-xylofuranosyl)guanine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
7,8,9,10-Tetrahydrobenzo[a]pyren-7-ol is a benzopyrene derivative that is activated by hepatic cytosol into electrophilic sulfuric acid esters[1], which are capable of forming covalent DNA adducts and inducing mutations[2].
Ethyl glycylmethioninate hydrochloride is a Methionine (HY-13694) derivative[1].
Glufosinate ammonium, a phosphinic acid analogue of glutamic acid, is an herbicide which is converted by plant cells into PT (L-phosphinothricin). Glufosinate ammonium exerts neurotoxic activity[1][2].
Daturaolone is a natural triterpenoid with anti-inflammatory and antinociceptive potentials. Daturaolone displays a COX-1 inhibitory activity[1].
Larotaxel (dihydrate) (XRP9881 (dihydrate)), a new taxane compound prepared by partial synthesis from 10-deacetyl baccatin III, is active against tumors[1].
Dicamba-5-aminopentanoic acid (DCc) is an immunizing and heterologous hapten, designed using the carboxylic acid group of dicamba to introduce a spacer arm for a better exposure of the herbicide's structure[1].
Murrayone, a coumarin-containing compound extracted from M. paniculata, is the most bioactive substance in this species and is a cancer metastasis chemopreventive agent based on its unique pharmacological properties[1].
Prolyl Hydroxylase inhibitor 1 (Compound 15i) is an orally active hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) inhibitor with an IC50 of 62.23 nM[1]. Antianemia agent[1].
KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels[1][2].
(+)-Lyoniresinol 3α-O-β-D-glucopyranoside (Compound 1) is a natural product that can be isolated from the bark of Aegle marmelos CORREA[1].
Tebanicline hydrochloride (ABT594 hydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM.
Ethyl phenylglyoxylate (Ethyl benzoylformate; Phenylglyoxylic acid ethyl ester) is the ethyl ester of phenylglyoxylic acid, used as a synthetic reagent[1].
Antimalarial agent 12 (compound R-3b) is a potent antimalarial agent. Antimalarial agent 12 shows growth inhibition on P. falciparum Dd2 Strain (EC50=155 nM), 3D7 strain (EC50=136 nM). Antimalarial agent 12 has CC50 values of 10,000 to 50,000 nM for HEK-293 and hPHep cell lines. Antimalarial agent 12 has a MIC of >250,000 nM for Escherichia coli[1].
(Rac)-PF-4136309 is an isoform of PF-4136309 (HY-13245), which is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.
Dermaseptin-B9 is an antimicrobial peptide isolated from frogs of the Phyllomedusinae subfamily[1].
Suplatast tosilate(IPD 1151T) is a Th2 cytokine inhibitor that attenuates IL-2, IL-5 and IL-13 production and has no effect on IFN-γ production. IC50 value:Target: Th2 cytokine inhibitorSuplatast Tosilate acts as an immunoregulator that suppresses IgE production, eosinophil infiltration and histamine release. Suplatast Tosilate(IPD 1151T) exhibits antiasthmatic, anti-inflammatory and antifibrotic activity in vivo and is orally active.
Endothelial lipase inhibitor-1 is a potent endothelial lipase inhibitor with an IC50 of 49 nM.
Midodrine is an α1-receptor agonist, for the treatment of dysautonomia and orthostatic hypotension.
13Z,16Z-Docosadienoic acid, a ω-6 polyunsaturated fatty acid, possesses anti-borreliae effect. 13Z,16Z-Docosadienoic acid, as a long-chain fatty acid (LCFA), is a free fatty acid receptor 4 (FFAR4 or GPR120, a LCFA receptor) agonist[1].
Bozitinib (PLB-1001) is a highly selective c-MET kinase inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) is a ATP-competitive small-molecule inhibitor, binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily[1].
Casanthranol is a concentrated mixture of anthranol glycosides from cascara sagrada (dried bark of Rhamnus p.) and used as a laxative in constipation and various medical conditions, stimulant laxative Casanthranol encourages bowel movements by acting on the intestinal wall to increase muscle contractions[1].
KN-92 is an inactive derivative of KN-93. KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM). IC50 value:Target: KN-92 is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM). KN-93 has been used to implicate roles for CaMKII in Ca2+-induced Ca2+ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca2+-dependent activation of HIF-1α in colon cancer cell.
(-)-Catechin gallate is a minor constituent in green tea catechins. (-)-Catechin gallate inhibits the activity of COX-1 and COX-2 enzymes.
Vogeloside is an iridoid that can be isolated from the roots of Triosteum pinnatifidum. Vogeloside inhibits nitric oxide production in LPS-activated macrophages[1].