These experiments discovered peptidomimetic fragments with inhibitory activity at millimolar concentrations.
Wilko Duprez, Prabhakar Bachu, Martin J Stoermer, Stephanie Tay, Róisín M McMahon,David P Fairlie, Jennifer L Martin 2015, 'Virtual Screening of Peptide and Peptidomimetic Fragments Targeted to Inhibit BacterialDithiol Oxidase DsbA.', PLoS ONEhttp://europepmc.org/articles/PMC4520593?pdf=render. Retrieved from PLOS CC BY 4.0 (https://creativecommons.org/licenses/by-sa/4.0/legalcode)
The topical application of minoxidil may achieve millimolar concentrations in the skin.
Soohwan Yum, Seongkeun Jeong, Dohoon Kim, Sunyoung Lee, Wooseong Kim, Jin-Wook Yoo,Jung-Ae Kim, Oh Sang Kwon, Dae-Duk Kim, Do Sik Min, Yunjin Jung 2017, 'Minoxidil Induction of VEGF Is Mediated by Inhibition of HIF-Prolyl Hydroxylase',International Journal of Molecular Scienceshttps://www.mdpi.com/1422-0067/19/1/53. Retrieved from DOAJ CC BY 4.0 (https://creativecommons.org/licenses/by-sa/4.0/legalcode)
The potencies of the known inhibitors range from low micromolar to millimolar concentrations.
Qianli Meng, Bingbing X. Li, Xiangshu Xiao 2018, 'Toward Developing Chemical Modulators of Hsp60 as Potential Therapeutics', Frontiers in Molecular Bioscienceshttp://journal.frontiersin.org/article/10.3389/fmolb.2018.00035/full. Retrieved from DOAJ CC BY 4.0 (https://creativecommons.org/licenses/by-sa/4.0/legalcode)
Inorganic anions were millimolar inhibitors, whereas diethyldithiocarbamate, sulfamate, sulfamide,phenylboronic acid, and phenylarsonic acid were micromolar ones.
Claudiu T. Supuran 2016, 'Legionella pneumophila Carbonic Anhydrases: Underexplored Antibacterial Drug Targets',Pathogenshttp://www.mdpi.com/2076-0817/5/2/44. Retrieved from DOAJ CC BY 4.0 (https://creativecommons.org/licenses/by-sa/4.0/legalcode)
Both polymers displayed a monotonous concentration dependence of their conductance in the analytically important sub-millimolar concentration range of ascorbic acid.
Svetlozar Ivanov, Vessela Tsakova, Vladimir M. Mirsky 2006, 'Conductometric transducing in electrocatalytical sensors: Detection of ascorbic acid',Electrochemistry Communicationshttp://www.sciencedirect.com/science/article/pii/S138824810600049X. Retrieved from DOAJ CC BY 4.0 (https://creativecommons.org/licenses/by-sa/4.0/legalcode)
The compound effects reported in the in vitro and in vivo analyses were obtained in the same millimolar concentration range.
Antonella Cotoia, Rosella Scrima, Julia V. Gefter, Claudia Piccoli, Gilda Cinnella,Michele Dambrosio, Mitchell P. Fink, Nazzareno Capitanio 2014, 'p-Hydroxyphenylpyruvate, an Intermediate of the Phe/Tyr Catabolism, Improves MitochondrialOxidative Metabolism under Stressing Conditions and Prolongs Survival in Rats Subjectedto Profound Hemorrhagic Shock', PLoS ONE10.1371/journal.pone.0090917. Retrieved from PLOS CC BY 4.0 (https://creativecommons.org/licenses/by-sa/4.0/legalcode)
Millimolar doses of tyramine inhibited glycerol release by adipocytes with a maximal antilipolytic effect comparable to that of insulin.
Francisco Les, Zsuzsa Iffiú-Soltész, Josep Mercarder, Christian Carpéné 2017, 'Tyramine activates lipid accumulation in rat adipocytes: influences of in vitroand in vivo administration', AIMS Molecular Sciencehttp://www.aimspress.com/Molecular/article/1596/fulltext.html. Retrieved from DOAJ CC BY 4.0 (https://creativecommons.org/licenses/by-sa/4.0/legalcode)
While the presented mechanochemical syntheses were carried out on the millimolar scale, they are easily scalable.
Laszlo Jicsinszky, Marina Caporaso, Katia Martina, Emanuela Calcio Gaudino, GiancarloCravotto 2016, 'Efficient mechanochemical synthesis of regioselective persubstituted cyclodextrins',Beilstein Journal of Organic Chemistryhttps://doi.org/10.3762/bjoc.12.230. Retrieved from DOAJ CC BY 4.0 (https://creativecommons.org/licenses/by-sa/4.0/legalcode)
However, affinity remained in the micromolar range, rather than the millimolar range associated with nonaffinityligands.
Huang X, He JX, Zhang HT, Sun K, Yang J, Wang HJ, Zhang HX, Guo ZZ, Zha ZG, Zhou CR 2017, 'Effect of dacarbazine on CD44 in live melanoma cells as measured by atomic force microscopy-basednanoscopy', International Journal of Nanomedicinehttps://www.dovepress.com/effect-of-dacarbazine-on-cd44-in-live-melanoma-cells-as-measured-by-at-peer-reviewed-article-IJN. Retrieved from DOAJ CC BY 4.0 (https://creativecommons.org/licenses/by-sa/4.0/legalcode)