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An enantiomer of (±)-atenolol; inhibits radioligand binding to β-ARs on sarcolemma-enriched membranes (Ki = 8.61 µM); has no effect on blood pressure in spontaneously hypertensive rats
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An indole-based SERM that binds to both ERα (IC50 = 26 nM) and ERβ (IC50 = 99 nM); antagonizes 17β-estradiol-dependent and hormone-independent growth of breast cancer cell proliferation (80% reduction with 10 nM) in a manner related to cell cycle arrest and downregulation of cyclin D1 and ERα
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A prodrug form of N-desethyl amodiaquine; active against several strains of P. falciparum in vitro (EC50s = 0.23-0.52 nM) and exhibits a synergistic effect when used in combination with N-desethyl amodiaquine; dose-dependently inhibits development of parasitemia in a mouse model of P. berghei infection
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A 15-carbon monounsaturated fatty acid; inhibits IFN-γ-induced production of kynurenine in THP-1 cells by 14%; has been used in studies of alternative β-oxidation pathways
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An allosteric activator of CD11b/CD18; increases K562 cell adhesion to fibrinogen (EC50 = 4 µM); reduces rolling velocity of leukocytes, decreasing the number of leukocytes recruited to injured tissue; anti-inflammatory in a zebrafish tailfin injury model and a mouse model of nephritis; competitively inhibits YopH (Ki = 1.94 µM) and anthrax lethal factor metalloproteinase (IC50 = 6 µM)
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A potent inhibitor of several NHE isoforms, inhibiting NHE1, NHE2, NHE3, and NHE5 with Ki values of 0.02, 0.5, 2.4, and 0.42 μM, respectively; less effectively inhibits NHE4 (IC50 ≥10 μM)
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An inhibitor of arginase types I and II; inhibits rat liver arginase I (Kis = 0.4 and 0.6 µM from kinetic analyses); inhibits human arginase II (Kis = 310 and 30 nM at pH 7.5 and 9.5, respectively); enhances nitric oxide-dependent relaxation of human penile corpus cavernosum smooth muscle in vitro at 0.1-1 mM
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A highly reactive 2-oxoaldehyde intermediate of the Maillard reaction produced during oxidative stress in response to excess sugar consumption and in association with diabetes; glycates and crosslinks proteins leading to the formation of advanced glycation endproducts
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An amino acid-containing building block; used in the synthesis of bis- and tris-branched carboxyl group-terminal PEGylating reagents; has been used in the synthesis of N3S chelators
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An inhibitor of EAAT1 and EAAT2 (IC50s = 22 and 17 nM for EAAT1 and EAAT2, respectively); selective for EAAT1 and EAAT2 over EAAT3 (IC50 = 300 nM), as well as a variety of neurotransmitter transporters and receptors at 10 µM; inhibits L-glutamate- and L-aspartate-induced currents in X. laevis oocytes at 10 µM; induces convulsions in mice at 0.2 UG/animal
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