|(S)-2-((((S)-3-(4-氯苯基)-4-苯基-4,5-二氢-1H-吡唑-1-基)(4-氯苯基磺胺基)亚甲基)氨基)-3-甲基丁酰胺|CsnPharm

CAS No.: 1392116-14-1

JD-5037 is a peripherally restricted CB1R antagonist with an IC50 of 1.5 nM.

规格	价格	促销价格	库存	数量

400-920-2911

加入购物车大规格询价

产品咨询

400-920-2911

纯度 & 质量文件批次:

生物活性

描述The cannabinoid 1 receptor (CB1R) is one of the most abundant G protein-coupled receptors (GPCRs) in the central nervous system, with key roles during neurotransmitter release and synaptic plasticity^[3]. JD5037 is a novel peripherally restricted CB1 receptor (CB1R) inverse agonist being developed for the treatment of visceral obesity and its metabolic complication, including nonalcoholic fatty liver disease and dyslipidemia. JD5037 was administered by oral gavage at 10, 40, and 150 mg/kg/day dose levels for up to 34 days to Sprague Dawley rats, and higher incidences of stereotypic behaviors were observed in 10 mg/kg females and 40 mg/kg males, and slower responses for reflex and sensory tests were observed only in males at 10 and 40 mg/kg during neurobehavioral testing. Results showed highest dose resulted in lower AUCs indicative of non-linear kinetics^[4]. JD5037 treatment of alcohol-drinking mice inhibits the formation of biologically active octanoyl-ghrelin without affecting its inactive precursor desacyl-ghrelin. In ghrelin-producing stomach cells, JD5037 reduced the level of the substrate octanoyl-carnitine generated from palmitoyl-carnitine by increasing fatty acid β-oxidation^[5].
参考文献

实验方案

技术信息

CAS号

1392116-14-1

储存条件

分子式

C27H27Cl2N5O3S

运输

蓝冰

分子量

572.51

别名

溶解度

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

请登录您的专属账户