中文名称: TDZD-8
英文名称: TDZD-8
CAS No: 327036-89-5
分子式: C10H10N2O2S
分子量: 222.26
T80005 TDZD-8 ≥98% (HPLC) (psaitong)
包装规格:
5mg 25mg 100mg in glass bottle
溶解性:
溶于DMSO( >10 mg/mL )
产品描述:

基本信息

产品编号:

T80005

产品名称:

TDZD-8 

CAS:

327036-89-5

 

储存条件

粉末

2-8℃

四年

 

 

分子式:

C10H10N2O2S

溶于液体

-80℃

6个月

分子量:

222.26

-20℃

1个月

化学名: 

4-Benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione

Solubility (25°C):

 

体外:

 

DMSO

44.5mg/mL (200.21mM)

Ethanol

44.5mg/mL (200.21mM)

Water

Insoluble

体内(现配现用):

1.请依序添加每种溶剂:10% DMSO40% PEG3005% Tween-8045% saline

Solubility:≥2.5mg/mL(11.25mM);Clear solution

此方案可获得 ≥ 2.5 mg/mL (11.25 mM,饱和度未知) 的澄清溶液。

1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

2.请依序添加每种溶剂:10% DMSO90%(20% SBE-β-CD in saline)

Solubility:≥2.5mg/mL(11.25mM);Clear solution

此方案可获得 ≥ 2.5 mg/mL (11.25 mM,饱和度未知) 的澄清溶液。

1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

3.请依序添加每种溶剂:10% DMSO90% corn oil

Solubility:≥2.5mg/mL(11.25mM);Clear solution

此方案可获得 ≥ 2.5 mg/mL (11.25 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

4.4992mL

22.4962mL

44.9924mL

5mM

0.8998mL

4.4992mL

8.9985mL

10mM

0.4499mL

2.2496mL

4.4992mL

 

生物活性

产品描述

一种选择性的GSK-3抑制剂。

靶点

GSK-3β 2μM (IC50)

 

体外研究

TDZD8 results in a significant decline of cellular ATP levels in PC-3 cells.TDZD8 (10μM) treatment also triggers a drastic autophagy response and AMPK activation in PC-3 cells.Furthermore,TDZD8 (10μM) reduces mTOR phosphorylation levels at the S2448 site.In addition,TDZD8 (10μM) induces LKB1 nuclear-cytoplasm translocation.

体内研究

TDZD-8 (TDZD8,1 or 2mg/kg,i.p.) both reduces the induction of p-DARPP32 following chronic L-dopa treatment in parkinsonian animals.TDZD8 treatment of 21 days induces a significant reduction in PKA expression in rats with established dyskinesia.Moreover,TDZD8 reduces FosB mRNA level in the striatum and lowers the expression of PPEB mRNA to similar levels as in 6-OHDA-lesioned rats without treated with L-dopa.The decrease in dyskinesia induced by TDZD8 is overcome by dopamine rceptor-1 agonist.

 

推荐实验方法(仅供参考)

激酶实验:

GSK-3 activity is assayed in 50 mM Tris-HCl, pH 7.5,10mM MgCl2,1mM EGTA,and 1mM EDTA buffer,at 37℃,in the presence of 15μM GS-1 (substrate),15μM [γ-32P]ATP in a final volume of 12μL.After 20 min incubation at 37℃,4μL aliquots of the supernatant are spotted onto 2×2 cm pieces of Whatman P81 phosphocellulose paper, and 20s later,the filters are washed four times (for at least 10 min each time) in 1% phosphoric acid.The dried filters are transferred into scintillation vials,and the radioactivity is measured in a liquid scintillation counter.Blank values are subtracted,and the GSK-3β activity is expressed in picomoles of phosphate incorporated in GS-1 per 20 min or in percentage of maximal activity.

 

动物实验:

 

Apomorphine hydrochloride is administered (0.5mg/kg).L-dopa (25mg/kg) plus benserazide-HCl (6.25mg/kg) are given once-daily.TDZD8,a non-ATP competitive inhibitor of GSK-3β,is dissolved in 10% DMSO and is administered i.p.(TDZD8-L group,1mg/kg;TDZD8-H group,2mg/kg,respectively) 30 min prior to L-dopa intake for 3 weeks.(±)-1-Phenyl-2,3,4,5-tetrahydro-(1H)-3-benzazepine-7,8-diol hydrochloride (SKF38393),a D1 Dopamine receptor agonist,is dissolved in saline and is administered i.p.(SKF38393-L group,5mg/kg;SKF38393-H group,10mg/kg,respectively) 30 min prior to L-dopa intake for 3 weeks.

 

保存条件:
2-8℃
UN码:
HazardClass:
危害声明:
安全说明:
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

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用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )

  • * = *

连续稀释计算器方程

  • 连续稀释

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  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):