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Thiodigalactoside (TDG), a non-metabolizable disaccharide, serves as an orally active, potent galectin (GAL) inhibitor, exhibiting Kd values of 24 μM and 49 μM for GAL1 and GAL3, respectively. Demonstrating anti-inflammatory and anti-cancer properties, it significantly diminishes body weight gain in diet-induced obese rats.

Samatasvir (ATOLIHZIXHZSBA-BTSKBWHGSA-N) is a pan-genotypic inhibitor of the HCV non-structural protein 5A.

Flucopride (Compound 4a) acts as an acetylcholinesterase inhibitor (AChE) with an IC50 value of 24 nM and serves as a partial agonist for the human 5-HT4 receptor (5-HT4R) with a Ki of 9.6 nM for (h)5-HT4R. It promotes non-amyloidogenic processing of APP in COS-7 cells transiently expressing (h)5-HT4R with an EC50 of 23.0 nM. Flucopride is also likely to exhibit significant gastrointestinal tract (GIT) penetration and blood-brain barrier (BBB) permeability, as determined in PAMPA experiments.

Tasimelteon (BMS-214778) is a melatonin receptor agonist that is used for the treatment of non-24 hour sleep-wake disorder in blind individuals.

(±)12-HEPE is produced by non-enzymatic oxidation of EPA, resulting in equal amounts of 12(S)-HEPE and 12(R)-HEPE. The biological activity of (±)12-HEPE is likely mediated by one of the individual isomers, primarily the 12(S) isomer in mammalian systems. 12-HEPE inhibits platelet aggregation with an IC50 of 24 μM, similar to 12-HETE (IC50 = 25 μM), and both compounds also inhibit U46619-induced contraction of rat aorta with IC50 values between 8.6-8.8 μM. [1][2]

6-Hydroxypyridin-3-ylboronic acid is a heterocyclic building block.1,2It has been used in the synthesis of non-nucleoside inhibitors of hepatitis C virus (HCV) RNA-dependent RNA polymerase nonstructural protein 5B (NS5B).16-Hydroxypyridin-3-ylboronic acid has also been used in the synthesis of mammalian target of rapamycin (mTOR) inhibitors.2 1.Hendricks, R.T., Spencer, S.R., Blake, J.F., et al.3-Hydroxyisoquinolines as inhibitors of HCV NS5b RNA-dependent RNA polymeraseBioorg. Med. Chem. Lett.19(2)410-414(2009) 2.Verheijen, J.C., Richard, D.J., Curran, K., et al.Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and sselective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 6-aryl substituentJ. Med. Chem.52(24)8010-8024(2009)

Isoprostanes are produced by the non-enzymatic, free radical peroxidation of phospholipid-esterified arachidonic acid. They have been used as biomarkers of oxidative stress, but they also have been found to have potent biological activity. ent-8-iso-15(S)-Prostaglandin F2α (ent-8-iso-15(S)-PGF2α) is a potent vasoconstrictor of porcine retinal and brain microvessels with EC50 values of 15 and 24 nM, respectively. This isoprostane is about ten-fold more potent than 8-iso-PGF2α in a whole blood platelet aggregation inhibition assay.

3,3'-((2-Chlorophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) is a non-nucleotide inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; Ki = 50 μM).1,2 It also inhibits urease (IC50 = 84.53 μM for the Jack bean enzyme).3 |1. Choudhary, M.I., Fatima, N., Khan, K.M., et al. New biscoumarin derivatives-cytotoxicity and enzyme inhibitory activities. Bioorg. Med. Chem. 14(23), 8066-8072 (2006).|2. Onyedibe, K.I., Wang, M., and Sintim, H.O. ENPP1, an old enzyme with new functions, and small molecule inhibitors - A STING in the tale of ENPP1. Molecules 24(22), E4192 (2019).|3. Khan, K.M., Iqbal, S., Lodhi, M.A., et al. Biscoumarin: New class of urease inhibitors; economical synthesis and activity. Bioorg. Med. Chem. 12(8), 1963-1968 (2004).

NO-indomethacin is a hybrid molecule of indomethacin and a nitric oxide (NO) donor. This drug design combines the anti-inflammatory properties of a non-steroidal anti-inflammatory drug (NSAID) with the gastrointestinal protective effects of NO. Compounds of this class retain their anti-inflammatory and analgesic activity, but have reduced gastrointestinal and kidney toxicity compared to the NSAID alone. NO-indomethacin also enhances the cancer chemopreventative activity of indomethacin. NO-indomethacin exhibits an IC50 of 82 μM, compared to >1,000 μM for indomethacin alone, for the inhibition of pancreatic cancer cell (PaCa-2) growth after 24 hours in culture.

PW0464 ((Rac)-Razpipadon) is a non-catechol D1R agonist and potent omplete G protein biased ligand with an EC50 (Gs-cAMP)=5.8 nM for the study of neurological disorders.

CAY10761 is an inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; IC50s = 467 and 429 μM for the human and snake venom enzymes, respectively).1,2 It also inhibits mushroom tyrosinase (Ki = 1.9 μM) and urease from jack bean, P. mirabilis, and B. pasteurii (IC50s = 0.093, <0.125, and 0.089 mM, respectively, at pH 8.2).3,4 |1. Khan, K.M., Fatima, N., Rasheed, M., et al. 1,3,4-Oxadiazole-2(3H)-thione and its analogues: A new class of non-competitive nucleotide pyrophosphatases/phosphodiesterases 1 inhibitors. Bioorg. Med. Chem. 17(22), 7816-7822 (2009).|2. Onyedibe, K.I., Wang, M., and Sintim, H.O. ENPP1, an old enzyme with new functions, and small molecule inhibitors - A STING in the tale of ENPP1. Molecules 24(22), E4192 (2019).|3. Ghani, U., and Ullah, N. New potent inhibitors of tyrosinase: Novel clues to binding of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides to the dicopper active site. Bioorg. Med. Chem. 18(11), 4042-4048 (2010).|4. Amtul, Z., Rasheed, M., Choudhary, M.I., et al. Kinetics of novel competitive inhibitors of urease enzymes by a focused library of oxadiazoles/thiadiazoles and triazoles. Biochem. Biophys. Res. Commun. 319(3), 1053-1063 (2004).

Dapivirine HCl is the salt form of Dapivirine, also known as TMC120, a non-nucleoside inhibitor for HIV reverse transcriptase with IC50 of 24 nM. The HIV-1 replication inhibitor dapivirine (DPV) is one of the most promising drug candidates being used in topical microbicide products for prevention of HIV-1 sexual transmission.

Tasimelteon-d5 is intended for use as an internal standard for the quantification of tasimelteon by GC- or LC-MS. Tasimelteon is a melatonin (MT) receptor agonist. It selectively binds MT1 and MT2 receptors over a panel of 160 additional receptors and enzymes at 10 µM. Tasimelteon inhibits forskolin-induced cAMP accumulation with EC50 values of 0.79 and 1 nM in NIH3T3 cells expressing the MT1 or MT2 receptor, respectively. Formulations containing tasimelteon have been used in the treatment of non-24-hour sleep-wake disorder.

Bupranolol is a non-selective beta blocker without intrinsic sympathomimetic activity (ISA), but with strong membrane stabilizing activity. Its potency is similar to propranolol. Bupranolol is quickly and completely absorbed from the gut. Over 90% undergo first-pass metabolism. Bupranolol has a plasma half life of about two to four hours, with levels never reaching 1 µg l in therapeutic doses. The main metabolite is carboxybupranolol, 4-chloro-3-[3-(1,1-dimethylethylamino)-2-hydroxy-propyloxy]benzoic acid – that is, the methyl group at the benzene ring is oxidized to a carboxyl group –, of which 88% are eliminated renally within 24 hours.

STING agonist-24 (CF504), a non-nucleotide small-molecule STING agonist, activates STING, leading to increased phosphorylation of STING, TBK1, and IRF3. It elevates levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells, demonstrating activity against SARS-CoV series strains [1].

CCK Octapeptide, non-sulfated acetate is a synthetic desulfated peptide of cholecystokinin.