GI 254023X
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260264-93-5
≥98%
A crystalline solid
391.5
(αr)-n-[(1s)-2,2-dimethyl-1-[(methylamino)carbonyl]propyl]-α-[(1s)-1-(formylhydroxyamino)ethyl]-benzenepentanamide, gi 4023, sri 028594
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- MSDS: View or download
An ADAM10 inhibitor (IC50 = 5.3 nM); selective for ADAM10 over ADAM17, MMP-1 and MMP-3 (IC50s = 541, 108, and 187 nM, respectively); inhibits MMP-9 and MMP-13 (IC50s = 2.5 and 1.1 nM, respectively); inhibits constitutive, but not PMA-induced shedding of CX3CL1 in COS-7 cells transfected with human chemokines (IC50s = 0.4 and >10 µM, respectively); inhibits constitutive, but not PMA-induced, secretion of IL-6R from THP-1 macrophages (IC50s = 1.8 and >10 µM, respectively); decreases Aβ42-induced shedding of LRP1 in HBMECs; increases Aβ42 transit across an in vitro blood brain barrier model; reduces brain LRP1 shedding and increases plasma levels of Aβ40 in a mouse model of Alzheimer's disease at 200 mg/kg
-20°C
