Bohemine served as a kinase inhibitor in the activation of bovine oocytes. Inhibition of DNA synthesis in oocytes was shown to be reversible, because after removal from boheminesupplemented medium the activated oocytes started to synthesize DNA. An attempt at elucidating the molecular basis of bohemine activity was undertaken through employing proteomics technology.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
Diverse effects of the cyclin-dependent kinase inhibitor bohemine: Concentration- and time-dependent suppression or stimulation of hybridoma culture
Franek F, et al. Cytotechnology. 2001 Jul;36(1-3): 117–123. PMID: 19003322.
In vivo metabolism of 2,6,9-trisubstituted purine-derived cyclin-dependent kinase inhibitor bohemine in mice: glucosidation as the principal metabolic route.
Chmela Z, et al. Drug Metab Dispos. 2001 Mar;29(3):326-34. PMID: 11181503.
7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells. IC50 value: 11 nM ([14C]-lactate influx).
7ACC1(DEAC; Coumarin D 1421; D 1421) selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.
Avibactam sodium is a covalent, reversible β-lactamase inhibitor, inhibits β-lactamase TEM-1 and CTX-M-15 with IC50 of 8 nM and 5 nM, respectively.
|AHU-377 hemicalcium salt
AHU-377 hemicalcium salt is a potent NEP inhibitor with an IC50 of 5 nM. AHU-377 is a component of the heart failure medicine LCZ696.
Isavuconazole is a moderate inhibitor of CYP3A4 and a water-soluble triazole with broad-spectrum antifungal activity.
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