产品名称

英文名称：AM251

同义词

AM251、183232-66-8、AM-251、AM 251、1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide、N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide、1h-pyrazole-3-carboxamide, 1-(2,4-d

产品性质

CAS编号：183232-66-8

分子式：C22H21Cl2IN4O

分子量：555.24

MDL号：MFCD01861181

PubChem编号：2125

英文别名：AM251|183232-66-8|AM-251|AM 251|1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide|N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide|1h-pyrazole-3-carboxamide, 1-(2,4-d

规格或纯度：≥98%

英文名称：AM251

生化机理：AM-251 is a 123I radioisotope and potent CB1 receptor antagonist derivative of the CB1 cannabinoid receptor inverse agonist SR141716A, presenting a radioprobe for in vivo binding studies at the CB1 receptor with a higher affinity (Ki = 7.49 nM) for CB1 than the parent compound (Ki = 11.5 nM). AM-251 has been employed in competitive binding studies to identify CB1 affinity of different cannabimimetic agonists in vivo. Characterization of AM-251-CB1 association with SPECT (single photon emission computed tomography) has been described. AM-251 is also a potent activator of the GPR55 receptor.Cannabinoid CB 1 receptor antagonist / inverse agonist (K i = 7.5 nM). Displays 306-fold selectivity over CB 2 receptors. Anorectic and antidepressant in vivo .

储存温度：2-8°C储存

运输条件：冰袋运输

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产品介绍：AM251是大麻素CB1受体拮抗剂，IC50为700 nM，在体内与小鼠脑CB1受体结合。An inverse agonist of the CB1 receptor; AM251, a CB1 cannabinoid receptor antagonist, has been used in a study to determine its interaction with hippocampal neurons to enhance spatial memory in mice.AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.An inverse agonist of the CB1 receptor; AM251, a CB1 cannabinoid receptor antagonist, has been used in a study to determine its interaction with hippocampal neurons to enhance spatial memory in mice.

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

INCHI：InChI=1S/C22H21Cl2IN4O/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-7-16(23)13-18(19)24)21(14)15-5-8-17(25)9-6-15/h5-10,13H,2-4,11-12H2,1H3,(H,27,30)

InChi Key：BUZAJRPLUGXRAB-UHFFFAOYSA-N

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

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

WGK Germany：3

PubChem CID：2125

Wikipedia：AM251

CAS Registry No.：183232-66-8

ChEMBL Ligand：CHEMBL285932

GPCRdb Ligand：AM251

溶解性：Soluble in DMSO (~10 mg/ml), ethanol (~10 mg/ml), DMF (~10 mg/ml), and 13 DMSOPBS (pH 7.2) (~14 mg/ml). Insoluble in water

敏感性：对热敏感

熔点：196-198°C

象形图：

信号词：Warning

危险声明：H315 Causes skin irritationH319 Causes serious eye irritationH335 May cause respiratory irritation

预防措施声明：P261,P305+P351+P338,P280,P302+P352,P321,P405,P501,P264,P271,P304+P340,P403+P233,P362+P364,P264+P265,P337+P317,P332+P317,P319

个人防护装备：dust mask type N95 (US)， Eyeshields， Gloves

产品包装