GI 254023X

GI 254023X

CAT N°: 28284
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From €85.00 €72.25

GI 254023X is an inhibitor of the metalloproteinase-disintegrin ADAM10 (IC50 = 5.3 nM).{50359} It is selective for ADAM10 over ADAM17, matrix metalloproteinase-1 (MMP-1), and MMP-3 (IC50s = 541, 108, and 187 nM, respectively), but also inhibits MMP-9 and MMP-13 (IC50s = 2.5 and 1.1 nM, respectively). GI 254023X inhibits constitutive shedding of CX3CL1, but not shedding induced by phorbol 12-myristate 13-acetate (PMA; Item No. 10008014), in COS-7 cells transfected with human chemokines (IC50s = 0.4 and >10 ?M, respectively). It also inhibits constitutive, but not PMA-induced, secretion of the IL-6 receptor (IL-6R) from THP-1 macrophages (IC50s = 1.8 and >10 ?M, respectively). GX 254023X (1 ?M) decreases shedding of low density lipoprotein receptor-related protein 1 (LRP1) induced by amyloid-? (1-42) (A?42; Item No. 20574) in human brain microvessel endothelial cells (HBMECs) and increases A?42 transit across an in vitro blood brain barrier model in a concentration-dependent manner.{50360} In vivo, GI 254023X (200 mg/kg) reduces brain LRP1 shedding and increases plasma levels of A?40 in a mouse model of Alzheimer’s disease.

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