AM251

目录号: GC15717纯度: >98.50%同义词: 1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-(哌啶-1-基)-1H-吡唑-3-甲酰胺

AM251是一种 1 型大麻素受体 (CB1) 拮抗剂，IC₅₀为8nM，同时也是G蛋白偶联受体55 (GPR55) 激动剂，其EC₅₀为39nM。

Cas No.: 183232-66-8

规格	价格	库存	数量
5mg	¥305.00	现货	1
10mg	¥494.00	现货	1
50mg	¥1,743.00	现货	1
500mg	¥10,458.00	现货	1
1g	¥18,795.00	现货	1

电话: 400-920-5774Email: sales@glpbio.cn

文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例

Nature
641, 529–536 (2025)
Nature
628, 630–638 (2024)
Nature
632, 686–694 (2024)
Nature
618, 1017–1023 (2023)
Nature
610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
Science
388(6745) (2025)
Science
387(6739) (2025)
Science
387(6734) (2025)
Cell Research
35, 97–116 (2025)
Cell Research
34, 683–706 (2024)
Cell Research
33, 273–287 (2023)
Cell Research
33, 546–561 (2023)
Cell Research
33, 904–922 (2023)
Cell Research
31, 1291–1307 (2021)

产品描述 Description

AM251 is a cannabinoid receptor type 1 (CB1) antagonist with an IC₅₀ of 8nM and a G protein-coupled receptor 55 (GPR55) agonist with an EC₅₀ of 39nM^{[1] [2]}. AM251 plays an important role in physiological processes such as cognition and immune function, and may be potentially valuable in the prevention and mitigation of fibrosis.

AM251 (10μM, 24hours) suppressed epithelial-mesenchymal transition of renal tubular epithelial cells without cytotoxicity^[3]. AM251 (10μM, 48hours) had an inhibitory effect on fibroblasts differentiation into myofibroblasts and collagen production induced by TGF-β in primary human fibroblasts cultures, with a pIC₅₀ of 5.5^[4]. AM251 (IC₅₀: 5μmol/L) induced apoptosis and G2/M cell cycle arrest in A375 human melanoma cells^[5].

AM251 (3mg/kg, i.p) treatment led to an increase in pro-inflammatory cytokines in rats, while decreasing fat pad mass and altering plasma hormone levels, inducing weight loss and adiposity reduction^[6]. AM251 (1mg/kg, i.p.) improved recognition memory in rats without alteration of their psychomotor activity and anxiety^[7]. AM251 (1mg/kg, i.p.) attenuated ataxia-related deficits in a cerebellar ataxia model, improved motor activity and blocked Purkinje cells neuronal degeneration in ataxic animals^[8].

References:
[1] Bruno A, Lembo F, Novellino E, Stornaiuolo M, Marinelli L. Beyond radio-displacement techniques for identification of CB1 ligands: the first application of a fluorescence-quenching assay. Sci Rep. 2014 Jan 20;4:3757. doi: 10.1038/srep03757. PMID: 24441508; PMCID: PMC3895875.
[2] Sharir H, Abood ME. Pharmacological characterization of GPR55, a putative cannabinoid receptor. Pharmacol Ther. 2010 Jun;126(3):301-13. doi: 10.1016/j.pharmthera.2010.02.004. Epub 2010 Mar 16. PMID: 20298715; PMCID: PMC2874616.
[3] Yoshinaga T, Uwabe K, Naito S, Higashino K, Nakano T, Numata Y, Kihara A. AM251 Suppresses Epithelial-Mesenchymal Transition of Renal Tubular Epithelial Cells. PLoS One. 2016 Dec 9;11(12):e0167848. doi: 10.1371/journal.pone.0167848. PMID: 27936102; PMCID: PMC5148003.
[4] Correia-Sá IB, Carvalho CM, Serrão PV, Machado VA, Carvalho SO, Marques M, Vieira-Coelho MA. AM251, a cannabinoid receptor 1 antagonist, prevents human fibroblasts differentiation and collagen deposition induced by TGF-β - An in vitro study. Eur J Pharmacol. 2021 Feb 5;892:173738. doi: 10.1016/j.ejphar.2020.173738. Epub 2020 Nov 19. PMID: 33220269.
[5] Carpi S, Fogli S, Romanini A, Pellegrino M, Adinolfi B, Podestà A, Costa B, Da Pozzo E, Martini C, Breschi MC, Nieri P. AM251 induces apoptosis and G2/M cell cycle arrest in A375 human melanoma cells. Anticancer Drugs. 2015 Aug;26(7):754-62. doi: 10.1097/CAD.0000000000000246. PMID: 25974027.
[6] O'Keefe L, Vu T, Simcocks AC, Jenkin KA, Mathai ML, Hryciw DH, Hutchinson DS, McAinch AJ. CB1 Ligand AM251 Induces Weight Loss and Fat Reduction in Addition to Increased Systemic Inflammation in Diet-Induced Obesity. Int J Mol Sci. 2022 Sep 28;23(19):11447. doi: 10.3390/ijms231911447. PMID: 36232744; PMCID: PMC9569643.
[7] Bialuk I, Winnicka MM. AM251, cannabinoids receptors ligand, improves recognition memory in rats. Pharmacol Rep. 2011;63(3):670-9. doi: 10.1016/s1734-1140(11)70578-3. PMID: 21857077.
[8] Ranjbar H, Soti M, Kohlmeier KA, Sheibani V, Ahmadi-Zeidabadi M, Rafiepour K, Shabani M. The cannabinoid antagonist, AM251 attenuates ataxia related deficiencies in a cerebellar ataxic model. Int J Neurosci. 2024 May;134(5):522-529. doi: 10.1080/00207454.2022.2126771. Epub 2022 Sep 30. PMID: 36120979.

AM251是一种 1 型大麻素受体 (CB1) 拮抗剂，IC₅₀为8nM，同时也是G蛋白偶联受体55 (GPR55) 激动剂，其EC₅₀为39nM^{[1] [2]}。AM251在认知和免疫功能等生理过程中发挥重要作用，在预防和缓解纤维化方面可能具有潜在价值。

AM251 (10μM，24hours) 可抑制肾小管上皮细胞的上皮-间质转化，且无细胞毒性^[3]。AM251 (10μM，48hours) 对原代人成纤维细胞培养物中由TGF-β诱导的成纤维细胞向肌成纤维细胞分化和胶原生成具有抑制作用，pIC₅₀为5.5^[4]。AM251 (IC₅₀：5μmol/L) 可诱导A375人黑色素瘤细胞凋亡和G2/M细胞周期停滞^[5]。

AM251 (3mg/kg, i.p) 可导致大鼠体内促炎细胞因子增加，同时减少脂肪垫质量并改变血浆激素水平，诱导体重下降和脂肪减少^[6]。AM251 (1mg/kg, i.p.) 可改善大鼠的识别记忆，但不会改变其精神运动活动和焦虑^[7]。AM251 (1mg/kg, i.p.) 可减轻小脑共济失调模型中与共济失调相关的缺陷，改善共济失调动物的运动活动并阻止Purkinje细胞神经元变性^[8]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:
Cell lines	Renal tubular epithelial cell line HK-2
Preparation Method	HK-2 cells were plated at 2 × 10⁴ cells per well on poly-D-lysine-coated 96-well plates overnight. TGF-β1 (2ng/ml) and AM251 (10μM) were incubated with the cells for 24h.
Reaction Conditions	10μM, 24hours
Applications	AM251 inhibited epithelial-mesenchymal transition in renal tubular epithelial cells, which informed the development of a novel therapeutic agent that inhibited EMT thereby preventing renal fibrosis.
Animal experiment [2]:
Animal models	Male Sprague Dawley rats
Preparation Method	Following the acclimatization period rats receive a high-fat diet (HFD) containing 40% digestible energy from lipids for 9 weeks. Animals were then maintained on the HFD and treated for a further six weeks with a daily i.p. injection, with 3mg/kg body weight of AM251 dissolved in the vehicle solution. Following treatment, rats were anesthetized with 3% isoflurane inhalation with each animal undergoing surgical removal of skeletal muscle, cardiac blood was then collected confirming death, with all other major organs including fat pads were removed post-mortem, weighed, and stored at −80 °C for further analyses.
Dosage form	3mg/kg, i.p., 6weeks
Applications	AM251 induced weight loss and fat reduction in addition to increased systemic inflammation in diet-induced obesity, the administration of AM251 increased systemic inflammation with increased levels of a wide range of cytokines.
References: [1] Yoshinaga T, Uwabe K, Naito S, Higashino K, Nakano T, Numata Y, Kihara A. AM251 Suppresses Epithelial-Mesenchymal Transition of Renal Tubular Epithelial Cells. PLoS One. 2016 Dec 9;11(12):e0167848. doi: 10.1371/journal.pone.0167848. PMID: 27936102; PMCID: PMC5148003. [2] O'Keefe L, Vu T, Simcocks AC, Jenkin KA, Mathai ML, Hryciw DH, Hutchinson DS, McAinch AJ. CB1 Ligand AM251 Induces Weight Loss and Fat Reduction in Addition to Increased Systemic Inflammation in Diet-Induced Obesity. Int J Mol Sci. 2022 Sep 28;23(19):11447. doi: 10.3390/ijms231911447. PMID: 36232744; PMCID: PMC9569643.

产品文档 Product Documents

批次：Purity:>98.50%

化学性质Chemical Properties

CAS 号

183232-66-8

同义词

1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-(哌啶-1-基)-1H-吡唑-3-甲酰胺

化学名

1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-piperidin-1-ylpyrazole-3-carboxamide

SMILES

CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)I

分子式

C₂₂H₂₁Cl₂IN₄O

分子量

555.24 g/mol

溶解性

≥ 55.5mg/mL in DMSO with gentle warming

保存条件

Store at -20°C

General tips

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。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

质量 (Mass)

体积 (Volume)

浓度 (Concentration)

分子量 (MW)

g/mol