AM251
Cat. No.:YN320988
产品名称: | AM251 |
CAS No.: | 183232-66-8 |
Chemical Name: | 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3-carboxamide |
Synonyms: | 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-piperidi |
分子量: | 555.24 |
分子式: | C₂₂H₂₁Cl₂IN₄O |
SMILES: | O=C(C1=NN(C2=CC=C(Cl)C=C2Cl)C(C3=CC=C(I)C=C3)=C1C)NN4CCCCC4 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | 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。 |
IC50和靶点: | |
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Selinsky, B.S., Gupta, K., Sharkey, C.T., et al.Structural analysis of NSAID binding by prostaglandin H2 synthase: Time-dependent and time-independent inhibitors elicit identical enzyme conformationsBiochemistry40(17),5172-5180(2001)
Ryberg, E., Larsson, N., Sjögren, S., et al.The orphan receptor GPR55 is a novel cannabinoid receptorBr. J. Pharmacol.152(7),1092-1101(2007)
Shearman, L.P., Rosko, K.M., Fleischer, R., et al.Antidepressant-like and anorectic effects of the cannabinoid CB1 receptor inverse agonist AM251 in miceBehav. Pharmacol.14(8),573-582(2003)
Baur, R., Gertsch, J., and Sigel, E.The cannabinoid CB1 receptor antagonists rimonabant (SR141716) and AM251 directly potentiate GABAA receptorsBr. J. Pharmacol.165(8),2479-2484(2012)
Yoshinaga, T., Uwabe, K., Naito, S., et al.AM251 suppresses epithelial-mesenchymal transition of renal tubular epithelial cellsPloS One11(12),e0167848(2016)
Carpi, S., Fogli, S., Romanini, A., et al.AM251 induces apoptosis and G2/M cell cycle arrest in A375 human melanoma cellsAnticancer Drugs26(7),754-762(2015)