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PRX-07034 HCl

    
10mM in DMSO

N-[1-(5-Chloro-2,3-dimethoxyphenyl)ethyl]-2-methylsulfonyl-5-piperazin-1-ylaniline hydrochloride

源叶(MedMol)
T28670 一键复制产品信息
903580-39-2
C21H29Cl2N3O4S
489.1256
PRX-07034; PRX07034; PRX 07034; PRX-07034 HCl; PRX-07034 hydrochloride.
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
T28670-1ml
10mM in DMSO

¥590.00

货期:3-5天 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
产品描述: PRX-07034 hydrochloride is a highly selective and potent 5-HT6 receptor antagonist with a Ki= 4-8 nM and an IC50 of 19 nM. PRX-07034 can be used for the research of enhancing working memory and cognitive flexibility
靶点: 5-HT6 Receptor:4-8 nM (Ki);5-HT6 Receptor:19 nM (IC50);5-HT1A Receptor:420 nM (Ki);5-HT1B Receptor:260 nM (Ki);5-HT1D Receptor:2.8 μM (Ki);5-HT2A Receptor:2.5 μM (IC50);5-HT2B Receptor:2.5 μM (IC50);5-HT2C Receptor:3.7 μM (IC50);Dopamine D3 Receptor:71 nM (Ki);Histamine H2 Receptor:0.64 μM (Ki);Opioid μ Receptor:0.45 μM (Ki)
体外研究: PRX-07034 is both a potent and highly selective 5-HT6 receptor antagonist (≥100-fold selectivity for the 5-HT6 receptor compared to 68 other GPCRs, ion channels, and transporters. PRX-07034 inhibits 5-HT1A, 5-HT1B, 5-HT1D, Dopamine D3, Histamine H2, and Opioid μ receptor with Kis of 420 nM, 260 nM, 2.8 µM, 71 nM, 0.64 µM, and 0.45 µM, respectively. PRX-07034 inhibits 5-HT2A, 5-HT2B, and 5-HT2C receptors with IC50s of 2.5 µM, 2.5 µM, and 3.7 µM, respectively.
In functional assays, PRX-07034 demonstrates low antagonist activity for the dopamine D3 receptor (IC50=4.8 µM) and very low agonistic activity for the opioid μ-receptor (EC50=19 µM) .
体内研究: PRX-07034 (0.1, 1, or 3 mg/kg; i.p.; 30 min prior to delayed spontaneous alternation testing) selectively enhances a switch to a place discrimination. Animal Model: Male Long-Evans rats weighing approximately 350 g Dosage: 0.1, 1, or 3 mg/kg Administration: Injected intraperitoneal Result: 1 and 3 mg/kg (but not 0.1 mg/kg) significantly enhanced delayed spontaneous alternation. The drug at 1 and 3 mg/kg also enhanced switching between a place and response strategy, but did not affect initial learning of either a place or response discrimination.
参考文献: 1. Eric G Mohler, et al. The effects of PRX-07034, a novel 5-HT6 antagonist, on cognitive flexibility and working memory in rats. Psychopharmacology (Berl). 2012 Apr;220(4):687-96.
溶解性: Soluble  in  DMSO、H2O
保存条件: -80℃(运输条件:冰袋低温运输)
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.044 ml 10.222 ml 20.445 ml
5 mM 0.409 ml 2.044 ml 4.089 ml
10 mM 0.204 ml 1.022 ml 2.044 ml
50 mM 0.041 ml 0.204 ml 0.409 ml
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