LP-211 - CAS:1052147-86-0 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	LP-211
英文名称:	LP-211
CAS No:	1052147-86-0	分子式:	C₃₀H₃₄N₄O	分子量:	466.62
CAS No:	1052147-86-0
分子式:	C₃₀H₃₄N₄O
分子量:	466.62

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L10396 LP-211 ≥98% (psaitong)

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包装规格：

100mg in glass bottle

溶解性：

溶于乙醇（50mg/mL 超声），溶于DMSO（100mg/mL 超声）

产品描述：

基本信息

产品编号：	L10396
产品名称：	LP-211
CAS:	1052147-86-0	储存条件	粉末	-20℃	四年

分子式：	C30H34N4O		溶于液体	-80℃	六个月
分子量	466.62			-20℃	一个月
化学名：	N-[(4-cyanophenyl)methyl]-6-[4-(2-phenylphenyl)piperazin-1-yl]hexanamide
Solubility (25°C)：
体外:	DMSO	100 mg/mL (214.31mM; Need ultrasonic)
	Ethanol	50 mg/mL (107.15mM; Need ultrasonic)
	Water
体内(现配现用):	请依序添加每种溶剂:10% DMSO→40% PEG300→5% Tween-80 →45% saline Solubility: ≥ 2.5 mg/mL (5.36mM); Clear solution
	此⽅案可获得 ≥ 2.5 mg/mL (5.36mM，饱和度未知) 的澄清溶液。以 1mL ⼯作液为例，取 100μL 25.0mg/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 50 μ L Tween-80，混合均匀；然后继续加⼊ 450μL ⽣理盐⽔定容⾄ 1mL。
	请依序添加每种溶剂:10% DMSO→90% (20% SBE-β-CD in saline) Solubility: ≥ 2.5 mg/mL (5.36mM); Clear solution
	此⽅案可获得 ≥ 2.5 mg/mL (5.36mM，饱和度未知) 的澄清溶液。以 1 mL 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。
	请依序添加每种溶剂:10% DMSO→90% corn oil Solubility: ≥ 2.5 mg/mL (5.36mM); Clear solution
	此⽅案可获得 ≥ 2.5mg/mL (5.36mM，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 25.0mg/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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.1431mL	10.7154mL	21.4307mL
5mM	0.4286mL	2.1431mL	4.2861mL
10mM	0.2143mL	1.0715mL	2.1431mL

生物活性

产品描述	一种选择性的，可透过血脑屏障的 5-HT7 受体激动剂，Ki 值为 0.58nM，选择性高于 5-HT1A 受体 (Ki，188nM) 和 D2 受体 (Ki，142nM)。
靶点	HT7 Receptor 0.58nM (Ki)	HT1A Receptor 188nM (Ki)	D2 Receptor 142nM (Ki)
体外研究	LP-211 is a selective 5-HT7 receptor agonist, with a Ki of 0.58nM, 324- and 245-fold selectivity over 5-HT1A receptor (Ki, 188nM) and D2 receptor (Ki, 142nM). LP-211 shows agonist properties with an EC50 of 0.6μM.
体内研究	LP-211 (10 mg/kg, i.p.) rapidly reaches the systemic circulation in the mouse, with mean Cmax of 0.76 ± 0.32μg/mL at 30 min. LP-211 (0.003-0.3 mg/kg, i.p.) significantly increases the micturition volume in a dose-dependent manner, and causes significant increases in voiding efficiency in spinal cord-injured (SCI) rats, and such effects can be completely reversed by SB269970. LP-211 (0.25 and 0.50 mg/kg i.p.) improves consolidation of chamber-shape memory in rats, resulting in significant novelty-induced hyperactivity and recognition.

推荐实验方法(仅供参考)

Kinase Assay

Binding of [3H]-LSD at rat cloned 5-HT7 receptor is performed in the assay. In 1mL of incubation buffer (50mM Tris, 10mM MgCl2 and 0.5mM EDTA, pH 7.4) are suspended 30μg of membranes, 2.5nM [3H]-LSD, LP-211 (6−9 concentrations). The samples are incubated for 60 min at 37°C. The incubation is stopped by rapid filtration on GF/A glass fiber filters (presoaked in 0.5% polyethylenimine for 30 min). The filters are washed with 3 × 53mL of ice-cold buffer (50mM Tris, pH 7.4). Nonspecific binding is determined in the presence of 10μM 5-CT. Approximately 90% of specific binding is determined under these conditions

Animal Administration

Rats
Thirty male adult Wistar rats (300-450 g) are assessed for novelty preference behavior after acute treatment (administered immediately after the training session and 24 h before the test session). After a 4 weeks' wash out, the rPDT is conducted to evaluate attraction from a greater/uncertain reward, with a sub-chronic treatment (five injections, immediately after sessions which follow the indifferent point). Food restriction, imposed by the experimenter through a limited quantity of food given at the end of each rPDT session, is applied to increase motivation to work for food delivery. All behavioral tests take place between 9:30 am and 4:00 pm. Rats are randomly assigned to treatment (LP-211 at 0.25 or 0.50 mg/kg i.p.) and control groups (injection volume 10mL/kg; n = 10 per group). The brain penetrant 5-HT7R agonist LP-211 is dissolved in a vehicle solution of 1% dimethyl sulfoxide (DMSO) in saline (0.9%NaCl). Control group receives the vehicle strictly in the same conditions.

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

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

质量 =

浓度 *

体积 *

分子量

*选择对应的单位 *空出希望得到的变量，填写另外两个变量

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
初始浓度:
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):

摩尔浓度计算公式

稀释公式

连续稀释计算器方程

连续稀释

计算结果