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Compound 3a was completely reduced to 7a after mixing with 10 mL-equiv DTE in dichloromethane for 20 min.
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Compound 3a was tested in two independent GTP-γS binding assays (n=4), and α-MSH was used as a positive control. Compound 3a showed increased binding (37.5±6.9% at 10 nM, 76.5±11.2% at 100 nM, and 106.5±11.8% at 1000 nM), comparable to the effect seen with α-MSH (33.5±3.1% at 10 nM, 84.0±11.1% at 100 nM, and 211.3±12.5% at 1000 nM).
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0011865299
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The pKa value for 3a was measured by pION, Inc., 5 Constitution Way, Woburn, MA 01801.
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