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ARN272

产品编号 T5357 CAS 488793-85-7

别名: ARN 272

ARN272 是大麻素转运抑制剂的一种。

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ARN272, CAS 488793-85-7

规格	价格/CNY	货期
2 mg	￥ 258	现货
5 mg	￥ 398	现货
10 mg	￥ 663	现货
25 mg	￥ 1,230	现货
50 mg	￥ 1,980	现货
100 mg	￥ 3,730	现货
200 mg	￥ 5,330	现货
1 mL * 10 mM (in DMSO)	￥ 455	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

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	FLAT inhibition by ARN272 appeared to be selective because the compound had little or no inhibitory activity on several endocannabinoid-metabolizing enzymes. Moreover, ARN272 produced only weak and incomplete inhibition of rat brain FAAH activity and was not significantly hydrolyzed after incubation with recombinant human FAAH-1 (≈5% hydrolysis after 24h at 37°C) [1].
体内活性	Administration of ARN272 (1 mg/kg, intraperitoneal, i.p.) in mice increased plasma levels of anandamide without changing the levels of 2-AG, OEA or PEA. The inhibitory effects of ARN272 on anandamide internalization in vitro and anandamide deactivation in vivo, along with the diminished anandamide accumulation observed in faah-1?/? mice [1]. The systemic administration of ARN272 produced a dose-dependent suppression of nausea-induced conditioned gaping in rats and produced a dose-dependent reduction of vomiting in shrews. The systemic co-administration of SR141716 with ARN272 (at 3.0?mg/kg) in rats produced a complete reversal of ARN272-suppressed gaping at 1.0?mg/kg. SR141716 alone did not differ from the vehicle solution [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
分子量	432.47
分子式	C27H20N4O2
CAS No.	488793-85-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: Insoluble

Ethanol: 8 mg/mL (18.50 mM)

DMSO: 50 mg/mL (115.61 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	2.3123 mL	11.5615 mL	23.123 mL	57.8075 mL
	5 mM	0.4625 mL	2.3123 mL	4.6246 mL	11.5615 mL
	10 mM	0.2312 mL	1.1561 mL	2.3123 mL	5.7807 mL
DMSO	20 mM	0.1156 mL	0.5781 mL	1.1561 mL	2.8904 mL
	50 mM	0.0462 mL	0.2312 mL	0.4625 mL	1.1561 mL
	100 mM	0.0231 mL	0.1156 mL	0.2312 mL	0.5781 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

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Fu J, et al. A catalytically silent FAAH-1 variant drives anandamide transport in neurons. Nat Neurosci. 2011 Nov 20;15(1):64-9. 2. O'Brien LD, et al. Anandamide transport inhibition by ARN272 attenuates nausea-induced behaviour in rats, and vomiting in shrews (Suncus murinus). Br J Pharmacol. 2013 Nov;170(5):1130-6.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

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：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 μL，一共给药动物10 只，您使用的配方为5% 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 μL DMSO (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：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：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

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

ARN272 488793-85-7 Metabolism Neuroscience FAAH ARN-272 inhibit Inhibitor ARN 272 inhibitor

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ARN272

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords