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AM251

目录号: PL09444 纯度: ≥98%

AM251是选择性大麻素1 (CB1) 受体拮抗剂，IC50 为8 nM。AM251也是 GPR55 的激动剂，EC50为39 nM。

CAS No. :183232-66-8

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中文名称	AM251
中文别名	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;1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-1-哌啶基-1H-吡唑-3-羧胺;5-正丙基乙内酰脲;AM251 抑制剂;1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-1-哌啶基-1H-吡唑-3-甲酰胺;AM251
英文名称	AM251
英文别名	1H-Pyrazole-3-carboxamide,1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-;AM 251;1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-piperidin-1-ylpyrazole-3-carboxamide;AM-251;1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3-carboxamide;Tocris-1117;1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide;AM 251 (pharmaceutical);N-(PIPERIDIN-1-YL)-5-(4-IODOPHENYL)-1-(2,4-DICHLOROPHENYL)-4-METHYL-1H-PYRAZOLE-3-CARBOXAMIDE;1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3-carboxamide AM251;AM-251 ,99%;1-(2,4-DICHLOROPHENYL)-5-(4-IODOPHENYL)-4-METHYL-N-1-PIPERIDINYL-1 H-PYRAZOLE-3-CARBOXAMIDE;1H-Pyrazole-3-carboxamide, 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-;AM251;3I4FA44MAI;CPD000466284;N-(Piperidin-1-yl)-5-
Cas No.	183232-66-8
分子式	C₂₂H₂₁Cl₂In₄O
分子量	555.24
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	AM251是选择性大麻素1 (CB1) 受体拮抗剂，IC50 为8 nM。AM251也是 GPR55 的激动剂，EC50为39 nM。

产品详情	AM251是选择性大麻素1 (CB1) 受体拮抗剂，IC₅₀ 为8 nM。AM251也是 GPR55 的激动剂，EC₅₀为39 nM。
生物活性	AM251 is a selective cannabinoid 1 (CB1) receptor antagonist with an IC 50 of 8 nM. AM251 also acts as a potent GPR55 agonist with an EC 50 of 39 nM.
性状	Solid
IC50 & Target[1][2]	IC50: 8 nM (CB1 receptor)
体外研究(In Vitro)	AM251 is a CB1 receptor antagonist/inverse agonist. AM251 produces an agonist response in HEK293 cells, similar to that found in the yeast expression system. AM-251 reduces cholesteryl ester synthesis in unstimulated and acetylated LDL-stimulated Raw 264.7 macrophages, CB2 and CB2 peritoneal macrophages. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	The CB1 antagonist AM251 (3 mg/kg, i.p.) decreases capsaicin-evoked nocifensive behavior. This suppressive effect is genotype dependent, and the interaction between the effects of genotype and AM251 approached significance. Planned comparisons reveal that AM251 reduces nocifensive behaviors in fatty-acid amide hydrolase (FAAH) KO mice (p<0.01) but fails to alter nocifensive behavior in WT mice (p>0.2) relative to their respective vehicle controls. AM251 (3 mg/kg, i.p.) reduces the duration of heat hypersensitivity in FAAH KO (F 1,9 =21.43, p<0.01) but not WT mice (p>0.3). AM251 suppresses capsaicin-evoked heat hypersensitivity in a time-dependent manner in FAAH KO (F 5,9 =4.349, p<0.01) but not in WT mice (p>0.3). Post-hoc analysis reveals that FAAH KO mice receiving vehicle (i.p.) display heightened thermal hypersensitivity at 30 (p<0.05
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Bruno A, et al. Beyond radio-displacement techniques for identification of CB1 ligands: the first application of afluorescence-quenching assay. Sci Rep. 2014 Jan 20;4:3757. [2]. Sharir H, et al. Pharmacological characterization of GPR55, a putative cannabinoid receptor. Pharmacol Ther. 2010 Jun;126(3):301-13.

溶解度数据	In Vitro: DMSO : 25 mg/mL (45.03 mM; Need ultrasonic)配制储备液

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[1]. Bruno A, et al. Beyond radio-displacement techniques for identification of CB1 ligands: the first application of afluorescence-quenching assay. Sci Rep. 2014 Jan 20;4:3757.
[2]. Sharir H, et al. Pharmacological characterization of GPR55, a putative cannabinoid receptor. Pharmacol Ther. 2010 Jun;126(3):301-13.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

AM251

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