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PRE-084 hydrochloride

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纯度: 99.54%

货号 T3198LCas号 75136-54-8

PRE-084 hydrochloride 是 σ1 的选择性激动剂在sigma 受体检测中,IC50值为44 nM。

PRE-084 hydrochloride
其他形式的 “PRE-084 hydrochloride”:

PRE-084 hydrochloride

一键复制产品信息
Rating icon 很棒

纯度: 99.54%

货号 T3198LCas号 75136-54-8

PRE-084 hydrochloride 是 σ1 的选择性激动剂在sigma 受体检测中,IC50值为44 nM。

规格价格库存数量
1 mg
¥ 160
现货
5 mg
¥ 363
现货
10 mg
¥ 586
现货
25 mg
¥ 1,200
现货
50 mg
¥ 2,350
现货
100 mg
¥ 3,500
现货
1 mL x 10 mM (in DMSO)
¥ 648
现货
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产品介绍


PRE-084 hydrochloride AI Summary
PRE-084 hydrochloride has been extensively tested for its bioactivities and has demonstrated a wide-ranging spectrum of effects. It shows potency in inhibiting the proliferation of various Plasmodium falciparum lines, with IC50 values ranging from 4466.8 nM to 14125.4 nM. Additionally, PRE-084 hydrochloride exhibits activity against endonuclease IV, the Menin-MLL interaction in leukemias, lipid storage modulation, histone lysine methyltransferase G9a, and delayed death inhibitors of the malarial parasite. It also affects HP1-beta chromodomain interactions with methylated histone tails, the human hERG channel, Marburg virus entry, Hepatitis C virus, and human tyrosyl-DNA phosphodiesterase 1 (TDP1), and induces synthetic lethality in 2HG-producing tumor cells. PRE-084 hydrochloride acts as an agonist at the sigma1 receptor in rat PC12 cells, enhancing NGF-induced neurite outgrowth by 27.5% and increasing neurite length by 181.3 um at 10 μM concentration over 5 days. This agonist activity persists in the presence of a sigma1 receptor antagonist BD-1063, albeit with reduced effectiveness, showing a decrease in neurite outgrowth by 16.0% and neurite length by 140.1 um. Similar trends are observed with another antagonist BD-1064, showing a decrease in neurite length by 23.0%. The compound exhibits high affinity for the sigma1 receptor with Ki values of 58.7 nM and 66.6 nM in the presence of DPH, but has significantly lower affinity (150.8 nM) in the DPH solvent. It shows minimal binding to kappa and delta opioid receptors, indicating selectivity towards sigma1 receptors under these assay conditions. Additionally, PRE-084 hydrochloride exhibits antiviral properties; it inhibits SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells, with inhibition rates of 17.53% and 1.21%, respectively, after 48 hours at 10 μM concentration, determined through high content imaging. Furthermore, it inhibits the SARS-CoV-2 3CL-Pro protease by 13.0% at a concentration of 20 µM as measured by a FRET-based assay..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
PRE-084 hydrochloride is a selective agonist of σ1(IC50:44 nM, in the sigma receptor assay).
化学信息
分子量353.88
分子式C19H28ClNO3
CAS No.75136-54-8
SmilesCl.O=C(OCCN1CCOCC1)C1(CCCCC1)c1ccccc1
密度no data available
颜色White
物理性状Solid
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
DMSO: 31 mg/mL (87.6 mM), Sonication is recommended.
H2O: 35.4 mg/mL (100.03 mM), Sonication and heating are recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.65 mM), Sonication is recommended.
请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。
溶液配制表
DMSO/H2O
1mg5mg10mg50mg
1 mM2.8258 mL14.1291 mL28.2582 mL141.2908 mL
5 mM0.5652 mL2.8258 mL5.6516 mL28.2582 mL
10 mM0.2826 mL1.4129 mL2.8258 mL14.1291 mL
20 mM0.1413 mL0.7065 mL1.4129 mL7.0645 mL
50 mM0.0565 mL0.2826 mL0.5652 mL2.8258 mL
H2O
1mg5mg10mg50mg
100 mM0.0283 mL0.1413 mL0.2826 mL1.4129 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments 比如您的给药剂量是10 mg/kg,每只动物体重20g,给药体积100 μLTargetMol | Animal experiments 一共给药动物10只,您使用的配方为5%TargetMol | reagent DMSO + 30%PEG300 + 5%Tween 80 + 60%Saline/PBS/ddH2O, 那么您的工作液浓度为2mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween80, 混匀澄清,再加 600μLSaline/PBS/ddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

方案所需的各类助溶剂如: DMSOPEG300 / PEG400Tween 80SBE-β-CD玉米油 等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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