A tamoxifen derivative, N, N-diethyl-2-[4-(phenylmethyl) phenoxy] ethanamine, selectively targets P-glycoprotein-positive multidrug resistant Chinese hamster cells
Recommended dosing of 1-2 mg subcutaneous injection 2-3x per week (6 mg/week total) compares to toxic dose estimated at ~22,500 mg (approximately 3,750 times higher than weekly dose)
Applications in Research As a molecular probe for studying short peptidemediated intracellular signalling Investigation of chromatin organisation, gene expression regulation, and telomere-associated processes in cell models In vitro studies examining peptidenucleus interactions and regulatory pathways As a reference compound in research involving pineal-derived peptide fragments Handling, Reconstitution & Stability Weigh under dry conditions
Relative to the wild-type enzyme, mutation of residue 15 to serine or alanine in UGT74F2 did not lessen the specific activity for SGE formation, but did increase the formation of SAG
Isoproterenol inhibits the increase in microvascular membrane permeability produced by bradykinin