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Org 27569

Org 27569

产品编号 T2635   CAS 868273-06-7

Org 27569 是一种 CB1 receptor 别构调节剂,可以增加激动剂与 CB1 结合,能够抑制激动剂诱导的 CB1 信号通路。

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Org 27569 Chemical Structure
Org 27569, CAS 868273-06-7
规格 价格/CNY 货期 数量
2 mg ¥ 232 现货
5 mg ¥ 418 现货
10 mg ¥ 672 现货
25 mg ¥ 1,420 现货
50 mg ¥ 2,750 现货
100 mg ¥ 3,970 现货
1 mL * 10 mM (in DMSO) ¥ 459 现货
产品目录号及名称: Org 27569 (T2635)
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纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Org 27569, an allosteric modulator of cannabinoid CB1 receptor, can induce a CB1 receptor state that is characterized by decreased inverse agonist affinity and enhanced agonist affinity.
体内活性 ORG 27569 (3.2 and 5.6 mg/kg, i.p.) markedly attenuates cocaine associated cue-induced reinstatement, cocaine priming-induced reinstatement, methamphetamine associated cue-induced reinstatement and methamphetamine priming-induced reinstatement in rat[4]. Org27569 (30 mg/kg, i.p.) produces CB1-independent hypophagic effects and does not affect the discriminative stimulus effects of anandamide (AEA). Org27569 (100 μg intracerebroventricularly) does not affect the pharmacologic effects of systemically administered CP55,940 compared with vehicle[5].
激酶实验 Equilibrium Binding Assays.: Binding assays are performed with the CB1 receptor agonist [3H]CP 55,940 (0.7 nM) and the CB1 receptor antagonist [3H]SR 141716A (1.2 nM), 1 mg/ml BSA and 50 mM Tris buffer containing 0.1 mM EDTA and 0.5 mM MgCl2, pH 7.4, in a total assay volume of 500 μl. Binding is initiated by the addition of mouse brain membranes (30 μg). Assays are carried out at 37°C for 60 min before termination by addition of ice-cold wash buffer (50 mM Tris buffer and 1 mg/ml BSA) and vacuum filtration using a 24-well sampling manifold and Whatman GF/B glass-fiber filters that have been soaked in wash buffer at 4°C for 24 h. Each reaction tube is washed five times with a 4-ml aliquot of buffer. The filters are oven-dried for 60 min and then placed in 5 ml of scintillation fluid, and radioactivity is quantitated by liquid scintillation spectrometry. Specific binding is defined as the difference between the binding that occurred in the presence and absence of 1 μM concentrations of the corresponding unlabeled ligand and is 70 to 80% of the total binding.
细胞实验 Cells expressing CB1 receptors are exposed to ORG27569 (10 μM) for 5 to 15 min. For toxin treatment to abrogate Gi coupling effects, PTX is added to the medium at 5 ng/ml. Following an 18-h incubation in the presence of toxin, cells are washed twice with PBS and treated with compounds. Cells are washed with ice-cold PBS, and cell lysates are obtained by harvesting the cells with ice-cold lysis buffer (150 mM NaCl, 1.0% IGEPAL CA-630, 0.5% sodium deoxycholate, 0.1% SDS, and 50 mM Tris, pH 7.5 containing 4-(2-aminoethyl)benzenesulfonyl fluoride, pepstatin A, E-64, bestatin, leupeptin, and aprotinin as protease inhibitors).(Only for Reference)
分子量 409.95
分子式 C24H28ClN3O
CAS No. 868273-06-7

存储

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

溶解度

DMSO: 41 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4393 mL 12.1966 mL 24.3932 mL 60.983 mL
5 mM 0.4879 mL 2.4393 mL 4.8786 mL 12.1966 mL
10 mM 0.2439 mL 1.2197 mL 2.4393 mL 6.0983 mL
20 mM 0.122 mL 0.6098 mL 1.2197 mL 3.0492 mL
50 mM 0.0488 mL 0.2439 mL 0.4879 mL 1.2197 mL
100 mM 0.0244 mL 0.122 mL 0.2439 mL 0.6098 mL

计算器

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稀释计算器
配液计算器
分子量计算器
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参考文献

1. Price MR, et al. Mol Pharmacol, 2005, 68(5), 1484-1495. 2. Ahn KH, et al. J Biol Chem, 2012, 287(15), 12070-12082. 3. Fay JF, et al. J Biol Chem, 2012, 287(40), 33873-33882. 4. Jing L, et al. Effects of the cannabinoid CB₁ receptor allosteric modulator ORG 27569 on reinstatement of cocaine- and methamphetamine-seeking behavior in rats. Drug Alcohol Depend. 2014 Oct 1;143:251-6. 5. Gamage TF, et al. In-vivo pharmacological evaluation of the CB1-receptor allosteric modulator Org-27569. Behav Pharmacol. 2014 Apr;25(2):182-5.
CB1 antagonist 1 CB1R/AMPK modulator 1 EHP-101 O-1602 2,3-Butanediol 2-Arachidonoylglycerol Hemopressin (rat) acetate(568588-77-2 free base) AEF0117

相关化合物库

该产品包含在如下化合物库中:
已知活性化合物库 活性脂质化合物库 抗COVID-19化合物库 经典已知活性库 抗阿尔茨海默症化合物库 抗肥胖化合物库 神经信号分子库 GPCR靶点分子库 表型筛选靶点鉴定库 神经退行性疾病化合物库

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
g
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。
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% ddH2O
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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

Org 27569 868273-06-7 GPCR/G Protein Cannabinoid Receptor Org27569 Inhibitor Org-27569 inhibit inhibitor

 

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