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GSK-3# Inhibitor XXIV 1PC X 5MG
Кат. №: 361567-5MG
Производитель: Sigma-Aldrich
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Товар оформляется под заказ
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GSK-3# Inhibitor XXIV 1PC X 5MG
Main image
Кат. №: 361567-5MG
Производитель: Sigma-Aldrich
Кол-во:
Фасовка:
Цена по запросу
Товар оформляется под заказ
Main image
Печать
GSK-3# Inhibitor XXIV 1PC X 5MG
Кат. №: 361567-5MG
Производитель: Sigma-Aldrich
Кол-во:
Фасовка:
Цена по запросу
Товар оформляется под заказ
Description General description The racemic mixture of a cell-permeable oxadiazolo-benzofuranylphenylsulfoxide that inhibits GSK-3β (IC50 = 35, 34, and 140 nM using the racemate, the (S), and the (R) enantiomer, respectively) in a highly selective manner as evidenced by its eutomer′s inability to inhibit 10 other serine/threonine and 12 other tyrosine kinases even at concentrations as high as 10 µM. Reported to exhibit good aqueous solubility (38 µg racemate/ml pH 6.8 buffer) and pharmacokinetic properties, being orally active in both rats and mice in vivo (Plasma AUC0-24h = 1380.6 and 457 ng•h/mL, respectively; 3 mg eutomer/kg via p.o.). The eutomer is also shown to be blood-brain-permeant in mice (brain AUC0-24h = 734 ng•h/mL; 3 mg/kg via p.o.) and oral dosing 30 min prior to CWS (cold water stress; 4 min below-neck inversion in 1-2 °C water) is demonstrated to reduce brain tau Thr205 phosphorylation (by 35%; 10 min post CWS) in mice in vivo. The racemic mixture of a cell-permeable oxadiazolo-benzofuranylphenylsulfoxide that inhibits GSK-3β (IC50 = 35, 34, and 140 nM using the racemate, the (S), and the (R) enantiomer, respectively) in a highly selective manner. The eutomer is shown to be orally active in rats and mice and significantly reduce CWS-induced brain tau Thr205 phosphorylation in mice in vivo. Packaging 5 mg in Glass bottle Packaged under inert gas Warning Toxicity: Standard Handling (A) Reconstitution Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. Other Notes Saitoh, M., et al. 2009. J. Med. Chem.52, 6270.; Description
Related Categories
Biochemicals and Reagents, D to K, Enzyme Inhibitors, Enzyme Inhibitors by Enzyme, Enzymes, Inhibitors, and Substrates, Glycogen synthase kinase More... Quality Level
Дорогой клиент, на сайте внедрена нейросеть для сбора информации о товаре. Это может привести к незначительным расхождениям в характеристиках продукции.
Description General description The racemic mixture of a cell-permeable oxadiazolo-benzofuranylphenylsulfoxide that inhibits GSK-3β (IC50 = 35, 34, and 140 nM using the racemate, the (S), and the (R) enantiomer, respectively) in a highly selective manner as evidenced by its eutomer′s inability to inhibit 10 other serine/threonine and 12 other tyrosine kinases even at concentrations as high as 10 µM. Reported to exhibit good aqueous solubility (38 µg racemate/ml pH 6.8 buffer) and pharmacokinetic properties, being orally active in both rats and mice in vivo (Plasma AUC0-24h = 1380.6 and 457 ng•h/mL, respectively; 3 mg eutomer/kg via p.o.). The eutomer is also shown to be blood-brain-permeant in mice (brain AUC0-24h = 734 ng•h/mL; 3 mg/kg via p.o.) and oral dosing 30 min prior to CWS (cold water stress; 4 min below-neck inversion in 1-2 °C water) is demonstrated to reduce brain tau Thr205 phosphorylation (by 35%; 10 min post CWS) in mice in vivo. The racemic mixture of a cell-permeable oxadiazolo-benzofuranylphenylsulfoxide that inhibits GSK-3β (IC50 = 35, 34, and 140 nM using the racemate, the (S), and the (R) enantiomer, respectively) in a highly selective manner. The eutomer is shown to be orally active in rats and mice and significantly reduce CWS-induced brain tau Thr205 phosphorylation in mice in vivo. Packaging 5 mg in Glass bottle Packaged under inert gas Warning Toxicity: Standard Handling (A) Reconstitution Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. Other Notes Saitoh, M., et al. 2009. J. Med. Chem.52, 6270.; Description
Related Categories
Biochemicals and Reagents, D to K, Enzyme Inhibitors, Enzyme Inhibitors by Enzyme, Enzymes, Inhibitors, and Substrates, Glycogen synthase kinase More... Quality Level
Дорогой клиент, на сайте внедрена нейросеть для сбора информации о товаре. Это может привести к незначительным расхождениям в характеристиках продукции.