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A prodrug form of temocaprilat; prevents impairment of acetylcholine-induced relaxation in aortic rings isolated from diabetic rats in a model of streptozotocin-induced diabetes; inhibits the angiotensin I-induced pressor response in normotensive rats at 0.1, 0.3, and 1 mg/kg; prevents coronary vascular remodeling induced by L-NAME in rats at 0.1 mg/ml in the drinking water; reduces plasma glucose levels in a KKAy mouse model of type 2 diabetes at 1 mg/kg
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A thiol-reactive fluorogenic probe; used to evaluate or quantify a variety of compounds containing reactive sulfur or thiol groups, including H2S, glutathione, proteins, and nucleotides
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A highly potent, reversible inhibitor of the EGFR (Ki = 5.2 pM; IC50 = 29 pM); rapidly suppresses autophosphorylation of EGFR in fibroblasts and human epidermoid carcinoma cells
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A flavonoid with diverse biological activities; induces QR in murine hepatoma cells (QR doubling concentration of 500 nM); inhibits TNF-α and IL-1β production in RAW 264.7 macrophages (IC50s = 17.28 and 23.5 μM, respectively) and in LPS-stimulated rats (48.6 and 55% reduction, respectively); shows selective cytotoxicity for CCRF-CEM leukemia cells (IC50 = 10.2 μM) in a panel of eight cancer cell lines (IC50s = >30 μM)
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A third-generation heterocyclic nitrogen-containing bisphosphonate that inhibits the prenylation of GTPases critical to the signaling events related to osteoclast-mediated bone resorption; has a high affinity for hydroxyapatite (Ki = 3.47 μM) and binds directly to mineralized bone where it decreases bone resorption by inhibiting osteoclast proliferation and inducing osteoclast apoptosis
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A modified nucleoside derived from 5-methylcytosine and is a minor constituent of RNA as well as DNA for certain organisms; used in epigenetics research, especially in studies involving DNA methylation processes
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A channel blocker that acts on several TRP channels, including TRPM2, TRPM8, and TRPC6 (IC50 = 1.7, 3.8, and 2.3 μM, respectively); inhibits PLA2, blocking the release of arachidonic acid when given at 50 μM
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An SSRI and a partial agonist of 5-HT1A (IC50 s = 0.2 and 0.5 nM, respectively); increases extracellular 5-HT in the rat ventral hippocampus and frontal cortex at 1 and 3 mg/kg, i.p.; decreases immobility in the forced swim test in both rats and mice at 1 mg/kg
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A μ- and κ-opioid receptor antagonist (Kis = 0.91 and 1.03 nM, respectively, in CHO membranes expressing the human receptors); selective for μ- and κ-opioid receptors over δ-opioid receptors (Ki = 13.26 nM in CHO membranes expressing the human receptors); decreases self-administration of alcohol in non-alcohol- and alcohol-dependent rats; reduces food and water intake and body weight in obese and lean rats at 25 mg/kg per day; inhibits morphine-induced scratching behavior and increases in the latency to tail withdrawal in a warm water tail withdrawal assay in rhesus monkeys at 32 UG/kg
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A complex of the tripeptide Gly-His-Lys and a copper(II) ion that has wound healing and anti-inflammatory activities; increases proliferation and the levels of collagen and secreted pro-MMP-2 in isolated human fibroblasts at 1 nM; increases levels of collagen, GAGs, and the expression of decorin in the wound tissue of rats at 2 mg; decreases LPS-induced increases in levels of ROS, IL-6, and TNF-α in RAW 264.7 cells at 10 µM; prevents LPS-induced decreases in lung SOD activity and GSH levels and reduces LPS-induced increases in the number of cells and the level of total protein in BALF in a mouse model of acute lung injury
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