AM251
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AM521是有效的大麻素受体1(CB1)拮抗剂,其IC50值与Ki值分别为8 nM和7.49 nM.
大麻素受体(CB1和CB2)属于G蛋白偶联受体,在各种生理过程中起着重要作用,如认知和免疫功能.
AM251抑制大麻素受体1激动剂与拮抗剂结合到大鼠脑膜[1].在海马中,2 μM AM251减弱内源性大麻素对GABA释放的抑制作用[2].1 μM AM 251抑制内源性大麻素信号对中间神经元放电的抑制[3].AM251抑制电压依赖性钠离子通道,降低神经元兴奋性,并抑制兴奋性与抑制性递质释放[4].
在大鼠的肥胖治疗中,AM251引起持续的食欲减退[5].此外,锻炼能使海马大麻素水平升高,促进记忆巩固,但AM251可以扰乱此过程[6].
参考文献：
[1] Lan, R, Q. Liu, P. Fan, S. Lin, S. R. Fernando, D. McCallion, R. Pertwee & A. Makriyannis: Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists. J. Med. Chem. 1999, 42, 769–776.
[2] Willow, M. & W. A. Catterall: Inhibition of binding of [3H]batrachotoxin A 20-α-benzoate to sodium channels by the anticonvulsant drugs diphenylhydantoin and carbamazepine. Mol. Pharmacol. 1982, 22, 627–635.
[3] Kreitzer, A. C., A. G. Carter & W. G. Regehr: Inhibition of interneuron firing extends the spread of endocannabinoid signaling in the cerebellum. Neuron 2002, 34, 787–796.
[4] Liao C, Zheng J, David LS, Nicholson RA. Inhibition of voltage-sensitive sodium channels by the cannabinoid 1 receptor antagonist AM 251 in mammalian brain. Basic Clin Pharmacol Toxicol. 2004 Feb;94(2):73-8.
[5] Chambers AP, Sharkey KA, Koopmans HS. Cannabinoid (CB)1 receptor antagonist, AM 251, causes a sustained reduction of daily food intake in the rat. Physiol Behav. 2004 Oct 15;82(5):863-9.
[6] de Oliveira Alvares L, de Oliveira LF, Camboim C, Diehl F, Genro BP, Lanziotti VB, Quillfeldt JA. Amnestic effect of intrahippocampal AM251, a CB1-selective blocker, in the inhibitory avoidance, but not in the open field habituation task, in rats. Neurobiol Learn Mem. 2005 Mar;83(2):119-24.
| Storage | Store at -20°C |
| M.Wt | 555.24 |
| Cas No. | 183232-66-8 |
| Formula | C22H21Cl2IN4O |
| Solubility | ≥55.5 mg/mL in DMSO with gentle warming; insoluble in H2O; ≥6.81 mg/mL in EtOH |
| Chemical Name | 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-piperidin-1-ylpyrazole-3-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)I |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 激酶实验 [1]: | |
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Caspase-3 试验 |
巨噬细胞接种(2×106/孔)于12孔培养板，加入DMSO 溶解的4 mM AM-251储备液，1小时后再加入乙醇溶解的2 mg/mL 7-酮基胆固醇，调节对照组，达到等体积的DMSO和乙醇。16小时后，测定caspase-3的活性。所有处理重复3次进行，数据以平均±标准误RFLU/mg蛋白质表示。 |
| 细胞实验 [2, 3]: | |
|
细胞系 |
人源黑色素瘤细胞A375; 264.7巨噬细胞 |
|
溶解方法 |
该化合物在DMSO中的溶解度> 10 mM。若配制更高浓度的溶液，一般步骤如下：请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
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反应时间 |
5 μM 处理48 h和72 h; 或 0.5、2 μM处理16 h |
|
应用 |
AM251 (5 μmol/l) 处理黑色素瘤细胞A375，诱导其凋亡、细胞周期停滞G2/M期并且增加cAMP 表达水平；同时，AM-251抑制7-酮基胆固醇介导的264.7巨噬细胞的凋亡。 |
| 动物实验 [3]: | |
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动物模型 |
成年雄性Sprague Dawley大鼠模型 |
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剂量 |
3 mg/kg，腹腔注射给药，持续1-4小时 |
|
应用 |
AM251处理大鼠增加对氧磷和毒死蜱氧的毒性；同时，AM-251 (1-4 μM)在体内抑制甾醇酯化；AM-251处理来源于野生型与CB2受体敲除小鼠的腹腔巨噬细胞能抑制乙酰化低密度脂蛋白刺激的胆固醇的酯化。 |
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注意事项 |
请于室内测试所有化合物的溶解度。实际溶解度和理论值可能略有不同，这是由实验系统的误差引起的，属于正常现象。 |
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References: 1. Thewke, D., Freeman-Anderson, N., Pickle, T., Netherland, C. and Chilton, C. (2009) AM-251 and SR144528 are acyl CoA:cholesterol acyltransferase inhibitors. Biochem Biophys Res Commun. 381, 181-186 2. Carpi, S., Fogli, S., Romanini, A., Pellegrino, M., Adinolfi, B., Podesta, A., Costa, B., Da Pozzo, E., Martini, C., Breschi, M. C. and Nieri, P. (2015) AM251 induces apoptosis and G2/M cell cycle arrest in A375 human melanoma cells. Anticancer Drugs. 26, 754-762 3. Liu, J. and Pope, C. (2015) The cannabinoid receptor antagonist AM251 increases paraoxon and chlorpyrifos oxon toxicity in rats. Neurotoxicology. 46, 12-18 |
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质量控制和MSDS
- 批次:
化学结构
相关生物数据
