產(chǎn)品目錄

規(guī)格	10mg 50mg 200mg
CAS	865854-05-3
別名
化學(xué)名	4-benzyl-2-naphthalen-1-yl-1,2,4-thiadiazolidine-3,5-dione
分子式	C19H14N2O2S
分子量	334.39
溶解度	≥ 16.7 mg/mL in DMSO with gentle warming
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

IC50: A potent, selective and irreversible non-ATP-competitive GSK-3β suppressor with an IC50 of 60 nM.

Tideglusib is a GSK-3 inhibitor currently undergoing phase II clinical trials for Alzheimer disease and progressive supranuclear palsy. Sustained oral administration of Tideglusib to animal models could down-regulates Tau hyper-phosphorylation, reduces brain amyloid plaque load, promotes learning and memory as well as prevents neuronal loss. [1]

In vitro: In vitro studies showed that after the unbound Tideglusib was removed from the reaction medium, the enzyme function could not be recovered. In addition, the dissociation rate constant of the reaction was as low as nearly zero. All above findings suggested that Tideglusib blocked GSK-3 irreversibly. Such irreversibility might be responsible for the non-competitive inhibition pattern with respect to ATP of Tideglusib and perhaps other structurally related compounds. [1]

In vivo: Based on double transgenic mice model co-expressing human mutant APP and tau, a study demonstrated that Tideglusib could suppress GSK-3, reduced amyloid and tau pathologies, blocked neuronal cell death and memory deficits in vivo. [2]

Clinical trial: A pilot, double-blind, placebo-controlled and randomized clinical trial was conducted to study the effect of Tideglusib in AD patients with an escalating dose. Thirty patients with mild to moderate AD were orally administered with Tideglusib in escalating doses of 400, 600, 800 and 1000 mg for periods of 4, 4, 6 and 6 weeks, respectively. This pilot study proved the safety and effectiveness of Tideglusib in AD patients. [3]

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請穿好實(shí)驗(yàn)服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

在線咨詢

留言注意事項(xiàng)：

1.遵守中華人民共和國有關(guān)法律、法規(guī)，尊重網(wǎng)上道德，承擔(dān)一切因您的行為而直接或間接引起的法律責(zé)任。

2.請您真實(shí)的反映產(chǎn)品的情況,不要捏造、誣蔑、造謠。如對產(chǎn)品有任何疑問,也可以留言咨詢。

3.未經(jīng)本站同意，任何人不得利用本留言簿發(fā)布個人或團(tuán)體的具有廣告性質(zhì)的信息或類似言論。

您感興趣的產(chǎn)品*
您的單位*
聯(lián)系人*
聯(lián)系電話*
詳細(xì)地址*
常用郵箱*
請輸入您對我們的意見或建議*
驗(yàn)證碼*