中文名称: 他克林盐酸盐水合物;他克林盐酸盐一水合物
英文名称: Tacrine hydrochloride (hydrate)
CAS No: 206658-92-6
分子式: C13H14N2?HCl?XH2O
分子量: 252.739882230759
T60028 他克林盐酸盐水合物;他克林盐酸盐一水合物 ≥98% (psaitong)
包装规格:
1g 5g in glass bottle
溶解性:
溶于DMSO(230mg/mL超声和加热)
产品描述:

基本信息

产品编号:

T60028

产品名称:

Tacrine hydrochloride (hydrate)

CAS:

206658-92-6

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C13H14N2?HCl?XH2O

溶于液体

-80℃

两年

分子量

252.74

-20℃

1个月

化学名: 

9-Amino-1,2,3,4-tetrahydroacridine hydrochloride hydrate

Solubility (25°C):

 

体外:

 

DMSO

50 mg/mL

Water

50 mg/mL

Ethanol

50 mg/mL

体内(现配现用):

1.请依序添加每种溶剂:10% DMSO→40% PEG300→5% Tween-80→45% saline

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

此⽅案可获得 ≥ 2.5 mg/mL (Infinity mM,饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例,取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中,混合均匀;向上述体系中加⼊ 50μL Tween-80,混合均匀;然后继续加⼊ 450μL ⽣理盐⽔定容⾄ 1mL。

2.请依序添加每种溶剂:10% DMSO→90% (20% SBE-β-CD in saline)

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

此⽅案可获得 ≥ 2.5 mg/mL (Infinity mM,饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例,取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL 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% DMSO→90% corn oil

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

此⽅案可获得 ≥ 2.5 mg/mL (Infinity 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。 以 1mL ⼯作液为例,取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL 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。

 

生物活性

产品描述

一种乙酰胆碱酯酶 (AChE) 和丁酰胆碱酯酶 (BChE) 的抑制剂。

靶点

IC50: 31nM (AChE), 25.6nM (BChE)

体外研究

Tacrine hydrochloride (hydrate) (12.5 to 37.5nM) inhibits venom acetylcholinesterase as well as human serum butyrylcholinesterase in a concentration-dependent manner. The IC50 is 31nM for snake venom AChE and 25.6nM for human BChE.

体内研究

Pretreatment with Tacrine hydrochloride (hydrate) also modifies absolute levels of cocaine self-administration during reacquisition. Body weight declines approximately one-half percent over four days of treatment with intravenous Tacrine hydrochloride (hydrate). Delivery of Tacrine hydrochloride (hydrate) by osmotic pump does not alter either linear- or repeated- cocaine-induced locomotor activity. There is no significant main effect or interaction with Tacrine hydrochloride (hydrate) treatment on active lever responding during reinstatement. Post hoc comparisons indicate that rats selfadministering cocaine has significantly lower alkaline phosphatase levels, relative to TTacrine hydrochloride (hydrate)- but not saline- treated rats evaluated by conditioned-place preference.

 

推荐实验方法(仅供参考)

Kinase Assay

The kinetic parameters of the interaction between Tacrine hydrochloride hydrate and cholinesterase are determined using the double reciprocal plot analyzed over a range of acetylthiocholine concentrations (0.05 to 1mM) in the absence and in the presence of Tacrine hydrochloride hydrate (12.5 to 37.5nM). IC50 is determined by percentage residual activity versus concentration of Tacrine hydrochloride hydrate

 

Animal Administration

Male Wistar rats at 9 weeks of age are used in this study. As soon as rats exhibit a stable pattern of self-administration under fixed-ratio-5 (FR-5) with a 20-second time out, sessions are discontinued over 24 hours and rats are left undisturbed in home cages, attached to a fluid swivel and steel-coil tether. This initial washout interval is assessed as more than adequate to allow clearance of plasma cocaine, which has a half-life of less than 20 minutes in rats. Beginning on the following day, 10 mg/kg-day of Tacrine hydrochloride hydrate or vehicle (saline) is administered as a chronic infusion over 4 days, delivered intravenously at 4.0 ml per day. After completion of these infusions, rats are then left undisturbed in home cages for an additional two days. This second washout period permits complete clearance of Tacrine hydrochloride hydrate, which has a half-life of less than two hours in rat brain. Cocaine self-administration is then re-initiated under FR-5 with a 20-second timeout period. To determine persistent effects of Tacrine hydrochloride hydrate, the pattern of self-administration is monitored over six additional sessions.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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摩尔浓度计算公式

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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