化学信息：
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化学名
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3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-dimethyl-1,2-oxazole-4-carboxamide
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简称
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TGR5
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别名
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TGR5 Receptor Agonist, CCDC, AOB2659, BDBM50414954, ZINC43208218
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中文名
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N/A
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化学式
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C18H14Cl2N2O2
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分子量
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361.22
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CAS号
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1197300-24-5
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纯度
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98%
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溶剂/溶解度
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Water<1mg/ml; DMSO40mg/ml; Ethanol40mg/ml
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溶液配制
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5mg加入1.38ml DMSO，或者每3.61mg加入1ml DMSO，配制成10mM溶液。SD2384-10mM用DMSO配制。
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生物信息：
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产品描述
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TGR5 Receptor Agonist, a potent TGR5(GPCR19) agonist, showed improved potency in the U2-OS cell assay (pEC50=6.8) and in melanophore cells (pEC50=7.5).
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信号通路
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GPCR & G Protein
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靶点
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TGR5
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－
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－
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－
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－
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IC50
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－
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－
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－
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－
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－
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体外研究
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TGR5 Receptor Agonist was profiled against more than 100 in-house and external 7TM, ion channel, enzyme, transporter, and nuclear hormone receptor selectivity assays, including FXR, another bile acid receptor, and showed significant response only in secretion of the pro-inflammatory cytokine TNFalpha (pIC50=6.8) in human primary monocytes following stimulation with LPS (lipopolysaccharide). In addition, TGR5 Receptor Agonist has good physicochemical properties and no measurable activity against three of the common cytochrome P450 (CYP450) isoforms (1A2, 2C9, and 2D6) or hERG dofetilide binding (pIC50<4.3).
In rat pharmacokinetic (PK) studies, however, TGR5 Receptor Agonist showed high in vivo clearance (Cl=85ml/min/kg) and intrinsic clearance (Clint=48ml/min/g) which provided a reasonable explanation for the observed poor exposure. Because the TGR5 receptor is expressed in the GI tract at levels that increase corresponding with L-cell population density, we believe that agonists such as 6 and 7 possessing poor systemic exposure are good tool compounds for directly targeting the TGR5 receptor in the GI tract via local administration (vide infra) rather than systemic exposure. Our hypothesis was that for this receptor, systemic exposure was not necessary to achieve the desired effect of stimulating GLP-1 secretion in vivo.
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体内研究
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N/A
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临床实验
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N/A
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特征
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N/A
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相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
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酶活性检测实验
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方法
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N/A
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细胞实验
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细胞系
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N/A
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浓度
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N/A
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处理时间
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N/A
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方法
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N/A
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动物实验
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动物模型
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N/A
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配制
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N/A
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剂量
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N/A
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给药方式
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N/A
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参考文献：
1. Evans KA, et al. J Med Chem. 2009 Dec 24, 52(24), 7962-5.
包装清单：
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产品编号
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产品名称
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包装
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SD2384-10mM
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TGR5 (GPCR19激动剂)
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10mM×0.2ml
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SD2384-5mg
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TGR5 (GPCR19激动剂)
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5mg
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SD2384-25mg
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TGR5 (GPCR19激动剂)
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25mg
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—
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说明书
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1份
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保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
注意事项：
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。
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