MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

AM251

CAS No. : 183232-66-8

MCE 站：AM251

产品活性：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。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Cannabinoid Receptor

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.

In Vivo: 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).

相关产品：Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Neuronal Signaling Compound Library  |  WIN 55,212-2 Mesylate  |  Rimonabant Hydrochloride  |  JD-5037  |  SR144528  |  2-Arachidonoylglycerol  |  6-Iodopravadoline  |  Pregnenolone  |  β-Caryophyllene  |  Olivetol  |  Olorinab  |  N-Oleoyl glycine  |  Org 27569  |  CB1 antagonist 2  |  TM38837  |  Yangonin  |  Taranabant ((1R,2R)stereoisomer)  |  MDA 19  |  BML-190  |  2-Palmitoylglycerol  |  AM281  |  BAY 38-7271  |  CB2R PAM  |  Hemopressin (human, mouse)  |  Hemopressin(rat)  |  Leelamine hydrochloride

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。