|
110165CBC O-GlcNAcase Inhibitor, TMG
(3aR,5R,6S,7R,7aR)-2-(Ethylamino)-3a,6,7,7a-tetrahydro-5-(hydroxymethyl)-5H-pyrano[3,2-d]thiazole-6,7-diol, 1,2-Dideoxy-2′-ethylamino-α-D-glucopyranoso-[2,1-d]-2′-thiazoline, OGA Inhibitor, Thiamet-G
China不适用
A cell-permeable, blood-brain barrier-permeant, orally active aminothiazoline that effectively increases O-GlcNAc level of cellular proteins both in cultures (EC50 = 30 nM, ECmax = 200 nM in PC3) in vitro and in rats (50 mg/kg i.v.; 200 mg/kg via drinking water ad libitum) and mice (500 mg/kg via drinking water ad libitum) in vivo by inhibiting O-GlcNAcase/OGA-mediated O-GlcNAc cleavage in a substrate-competitive (Ki = 21 nM), time- and dose-dependent, and highly selective manner. TMG long-term treatment in murine AD model effectively prevents loss of motor neurons and reduces NFTs in brain without apparent effect on Tau hyperphosphorylation. O-GlcNAcylation is also reported to slow down heat-induced sTAB1 (TAK1-binding protein) aggregation and modulate CK2α kinase activity and substrate selectivity in vitro.
产品信息
Form Off-white solid
Molar mass 248.3
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥98% by HPLC
Solubility DMSO or H2O
Chemical formula C9H16N2O4S
CAS number 1009816-48-1
商店和运输信息
Storage -20°C
Ship Ambient Temperature Only
Harmful |