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ARN272

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产品编号 T5357Cas号 488793-85-7
别名 ARN 272

ARN272 是大麻素转运抑制剂的一种。

ARN272
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ARN272

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纯度: 98.23%
产品编号 T5357 别名 ARN 272Cas号 488793-85-7

ARN272 是大麻素转运抑制剂的一种。

规格价格库存数量
2 mg¥ 125现货
5 mg¥ 197现货
10 mg¥ 347现货
25 mg¥ 696现货
50 mg¥ 1,120现货
100 mg¥ 1,780现货
200 mg¥ 2,580现货
1 mL x 10 mM (in DMSO)¥ 223现货
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产品介绍

生物活性
产品描述
ARN272 is a FAAH-like anandamide transporter (FLAT) inhibitor (IC50: 1.8 μM).
靶点活性
Anandamide transporter:1.8 μM
体外活性
ARN272对FLAT的抑制似乎是选择性的,因为这种化合物对几种内源性大麻素代谢酶几乎没有或没有抑制作用。此外,ARN272对大鼠脑FAAH活性的抑制作用弱且不完全,且在与重组人FAAH-1孵育后不被显著水解(在37°C下孵育24小时后的水解率约为5%)[1]。
体内活性
在小鼠体内,通过腹腔注射ARN272(1mg/kg)能够提高血浆中阿纳米酰胺(anandamide)的水平,而不影响2-AG、OEA或PEA的水平。研究指出,ARN272抑制阿纳米酰胺在体外内化和在体内失活的效应,以及在faah-1/ 小鼠中观察到的阿纳米酰胺积聚减少现象[1]。ARN272的系统性给药在大鼠中产生了剂量依赖性地抑制因恶心引起的条件性张口行为,并在鼩鼱中减少了呕吐的剂量依赖性降低。在大鼠中,与ARN272(3.0mg/kg)的系统性共同给药能完全逆转ARN272以1.0mg/kg抑制的张口行为。SR141716单独使用的效果与载体溶液无差异[2]。
动物实验
All rats were surgically implanted with intra-oral cannula under isoflurane anaesthesia. Following recovery from surgery (3 days), rats received a single adaptation trial to habituate them to the chamber and the infusion procedure. During the adaptation trial, rats were placed individually in the TR chamber and received a 2?min intra-oral infusion of water (reverse osmosis water infused at 1?mL/min). On the following day, rats received the first of two conditioning trials (separated by 72?h). On each conditioning trial, rats received a pretreatment injection of ARN272 or VEH 120?min prior to the conditioning trials. During conditioning trails, rats were intra-orally infused with a saccharin solution (0.1%) for 2?min (1?mL/min) and orofacial and somatic reactions were recorded on video. Immediately following the saccharin infusion, the rats were injected with LiCl (0.15?M) or saline, and then returned to their home cage. Two additional groups were added (after ARN272 at 3.0?mg·kg?1 attenuated gaping) where pretreatment of ARN272 at 3.0?mg·kg?1 or VEH was given 120?min prior, and with SR141716 30?min prior, to each conditioning trial. The groups were VEH-Saline (VEH-SAL), n = 9; VEH-LiCl, n = 8; 0.1?mg/kg ARN272-LiCl, n = 9; 1.0?mg/kg ARN272-LiCl, n = 8; 3.0?mg/kg ARN272-LiCl, n = 8; 1.0?mg/kg SR-3.0?mg/kg ARN272, n = 8; 1.0?mg/kg SR-VEH, n = 8. Seventy-two hours following the second conditioning trial, the rats received a drug-free TR test. During the TR test, rats were re-exposed to a 2?min intra-oral infusion of saccharin solution and their orofacial and somatic responses again recorded. All video recordings were later scored by a rater blind to the experimental conditions using ‘The Observer'. Following the TR test, the rats were returned to their home cages and at 16:00?h, their water bottles were removed to begin a water deprivation regime in preparation for the CTA test.At 08:00?h the following morning, the rats received a one-bottle test in which a graduated tube of 0.1% saccharin solution was placed on the home cage, and the amount consumed was recorded at 30 and 120?min intervals. A one-bottle test was used as there is evidence to suggest it is more sensitive in detecting between-group differences in strength of taste avoidance than a two-bottle test where both water and saccharin are made available [2].
别名ARN 272
化学信息
分子量432.47
分子式C27H20N4O2
CAS No.488793-85-7
SmilesOc1ccc(cc1)-c1nnc(Nc2ccc(cc2)C(=O)Nc2ccccc2)c2ccccc12
密度no data available
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
H2O: Insoluble
Ethanol: 8 mg/mL (18.50 mM)
DMSO: 50 mg/mL (115.61 mM)
溶液配制表
1mg5mg10mg50mg
1 mM2.3123 mL11.5615 mL23.1230 mL115.6150 mL
5 mM0.4625 mL2.3123 mL4.6246 mL23.1230 mL
10 mM0.2312 mL1.1561 mL2.3123 mL11.5615 mL
1mg5mg10mg50mg
20 mM0.1156 mL0.5781 mL1.1561 mL5.7807 mL
50 mM0.0462 mL0.2312 mL0.4625 mL2.3123 mL
100 mM0.0231 mL0.1156 mL0.2312 mL1.1561 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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