Chemical Structure : ASN90
CAS No.: 1884154-02-2
货号: PC-73139Not For Human Use, Lab Use Only.
ASN90 is a potent, selective, substrate-competitive O-GlcNAcase (OGA) inhibitor with IC50 of 10.2 nM.
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ASN90 is a potent, selective, substrate-competitive O-GlcNAcase (OGA) inhibitor with IC50 of 10.2 nM.
ASN90 does not inhibit hexosaminidase (Hex).
ASN90 induced protein O-GlcNAcylation in plated human and rodent PBMC with similar potencies (EC50 of 209 and 489 nM for human and rodent PBMC, respectively).
ASN90 is chemically distinct from carbohydrate-type substrate mimetic OGA inhibitors such as Thiamet G and MK-8719. ASN90 binds to the OGA enzyme in the living rat brain and robustly elevates the O-GlcNAcylation of brain proteins, including both tau and α-synuclein, in vivo.
ASN90 exhibited therapeutic efficacy in preclinical models of both tau and α-synuclein pathology.
分子量 | 375.447 | |
分子式 | C17H21N5O3S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
(S)-N-(5-(4-(1-(benzo[d][1,3]dioxol-5-yl)ethyl)piperazin-1-yl)-1,3,4-thiadiazol-2-yl)acetamide |
1. Permanne B, et al. ACS Chem Neurosci. doi: 10.1021/acschemneuro.2c00057.
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