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A semisynthetic macrocyclic lactone prepared by the oxidation and oximation of an 80:20 ratio of milbemycin A3 and A4; nematocide and insecticide activity via the potentiation of glutamate and GABA-gated chloride-channel opening
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An analog of dapagliflozin that displays similar selectivity for inhibiting SGLT2 over SGLT1 (Kis = 5.3 and 330 nM, respectively); significantly reduces phlorizin-sensitive sugar transport in COS-1 cells expressing human SGLT2
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An AGE, produced by the oxidative modification of glycated proteins during oxidative stress; increases with aging and during pathologies marked by oxidative stress; activates RAGE, triggering signaling through MAPKs and NF-κB
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A selective FLT3 inhibitor (Kd = 1.6 nM) that inhibits the proliferation of MV4-11 cells both in vitro (IC50 = 0.56 nM) and in in vivo mouse models of FLT3-ITD acute myeloid leukemia
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An orally-active quinoline-3-carboxamide that inhibits tumor angiogenesis and supplements radiation or chemotherapy in animal models of prostate cancer
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A secondary metabolite produced by some species of lichen that binds FAS-II enzymes to produce antibacterial and antiplasmodial effects; inhibits PfFabZ and PfFabI (IC50 = 10.7 and 36.1 µM, respectively) but shows low efficacy against the malaria parasite P. berghei (IC50 = 77.3 µM)
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A dihydropyridine that acts as a potent, selective α1A-adrenoceptor antagonist (Ki = 0.16 nM); less potently blocks L- and T-type Ca2+ channels (IC50s = 0.4 and 0.9 µM, respectively)
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Active metabolite of molsidomine that acts as a potent vasorelaxant and inhibitor of platelet aggregation; produces both NO and superoxide to generate peroxynitrite under physiological conditions
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A relatively selective inhibitor of iNOS, exhibiting IC50 values of 0.4-3.3 µM for iNOS as opposed to 8-38 and 17-92 µM for eNOS and nNOS, respectively; effectively inhibits iNOS both in vitro and in vivo
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DETA NONOate is a NO donor. It spontaneously dissociates in a pH-dependent, first-order process with a half-life of 20 hours and 56 hours at 37°C and 22-25°C, pH 7.4, respectively, to liberate 2 moles of NO per mole of parent compound.{1190,5437}
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One of several nitroaniline fatty acid amides that can be used to measure FAAH activity; exposure to FAAH results in the release of the yellow colorimetric dye m-nitroaniline (ε = 13,500 at 410 nm) allowing for fast and convenient measurement of FAAH activity using a 96-well plate spectrophotometer
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