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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-(哌啶-1-基)-1H-吡唑-3-甲酰胺 更多供应商
公司名称: 北京百灵威科技有限公司  
联系电话: 400-666-7788 010-82848833
产品介绍: 英文名称:AM 251
CAS:183232-66-8
纯度:99% 包装信息:10Mg,250Mg,25Mg 备注:化学试剂、精细化学品、医药中间体、材料中间体
公司名称: 武汉易泰科技有限公司上海分公司  
联系电话: 18930552037 821-50328103-801
产品介绍: 中文名称: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
英文名称:AM 251;N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-Methyl-1H-pyrazole-3-carboxaMide
CAS:183232-66-8
纯度:99% HPLC 包装信息:1Mg ; 5Mg;10Mg ;100Mg;250Mg ;500Mg ;1g;2.5g ;5g ;10g
公司名称: Ascent Scientific  
联系电话: 4401179829988
产品介绍: 英文名称:AM 251
CAS:183232-66-8
纯度:>99% 包装信息:10mg;50mg 备注:CB1 receptor antagonist / inverse agonist
公司名称: VDM Biochemicals   
联系电话: 0330-2528181
产品介绍: 英文名称:AM 251
CAS:183232-66-8
纯度:>=98%
公司名称: 凯试(上海)科技有限公司  
联系电话: 021-50135380
产品介绍: 英文名称:AM 251
CAS:183232-66-8
纯度:98% 备注:1500元/10mg; 1950元/25mg; 12000元/250mg
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
生物活性靶点体外研究体内研究 MSDS 用途与合成方法 1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-(哌啶-1-基)-1H-吡唑-3-甲酰胺价格(试剂级) 上下游产品信息
中文名称: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
中文同义词: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;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
英文名称:AM 251
英文同义词:AM 251;1-(2,4-DICHLOROPHENYL)-5-(4-IODOPHENYL)-4-METHYL-N-1-PIPERIDINYL-1 H-PYRAZOLE-3-CARBOXAMIDE;N-(PIPERIDIN-1-YL)-5-(4-IODOPHENYL)-1-(2,4-DICHLOROPHENYL)-4-METHYL-1H-PYRAZOLE-3-CARBOXAMIDE;AM-251 ,99%;CS-985;AM 251 NEW;AM 251 (pharmaceutical);1H-Pyrazole-3-carboxamide, 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-
CAS号:183232-66-8
分子式:C22H21Cl2IN4O
分子量:555.24
EINECS号:
相关类别:小分子抑制剂;G蛋白偶联受体&G蛋白;小分子抑制剂,天然产物;Inhibitors;Cannabinoid receptor;Cannabinoid;Aromatics;Heterocycles;Cannabinoids
Mol文件:183232-66-8.mol
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-(哌啶-1-基)-1H-吡唑-3-甲酰胺 性质
熔点 195-196℃
密度 1.65±0.1 g/cm3(Predicted)
储存条件 Store at RT
溶解度 DMSO: >10 mg/mL, soluble
形态solid
酸度系数(pKa)11.31±0.20(Predicted)
颜色white
CAS 数据库183232-66-8
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 用途与合成方法
生物活性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。
靶点

IC50: 8 nM (CB1 receptor)

体外研究

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.

体内研究

The CB1 antagonist AM251 (3 mg/kg, i.p.) decreases capsaicin-evoked nocifensive behavior (F 1,18 =28.45, p<0.0001). This suppressive effect is genotype dependent (F 1,18 =14.83, p<0.01), and the interaction between the effects of genotype and AM251 approached significance (F 1,18 =4.704, p=0.0587). 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), 60 (p<0.05), and 90 (p<0.001) minutes post-capsaicin in comparison to FAAH KO animals receiving AM251). One-way ANOVA shows that AM251 (AM-251) injected into the rats significantly decreases both of the percentage of entries in the open arms and time spent in the open arms, compare to controls. The Tukey-Kramer test analysis reveals a significant reduction for the doses of 1 mg/kg (P<0.05) and 5 mg/kg (P<0.01) compare to control rats in the time spent in the open arms. Also, AM251 significantly decreases percentage of entries in the open arms for the doses of 1 and 5 mg/kg (P<0.05).

安全信息
危险品标志 Xi
危险类别码 36/37/38
安全说明 26-36
WGK Germany 3
MSDS信息
提供商语言
SigmaAldrich 英文
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 价格(试剂级)
更新日期产品编号产品名称CAS编号包装价格
2021/01/25A3151AM 251
AM 251
183232-66-810mg660元
2021/01/25A3151AM 251
AM 251
183232-66-850mg1990元
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