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GATA4-NKX2-5-IN-1

货号 T11368Cas号 544681-96-1 一键复制产品信息纯度: 99.65%
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GATA4-NKX2-5-IN-1 剂量依赖性地抑制 GATA4–NKX2-5转录协同作用(IC50:3 μM),但不影响参与调节 GATA4 磷酸化的蛋白激酶的活性。它能够调节肥大激动剂诱导的心脏基因表达。

GATA4-NKX2-5-IN-1

一键复制产品信息
Rating icon 很棒

纯度: 99.65%

货号 T11368Cas号 544681-96-1

GATA4-NKX2-5-IN-1 剂量依赖性地抑制 GATA4–NKX2-5转录协同作用(IC50:3 μM),但不影响参与调节 GATA4 磷酸化的蛋白激酶的活性。它能够调节肥大激动剂诱导的心脏基因表达。

GATA4-NKX2-5-IN-1
规格价格库存数量
1 mg
¥ 333
现货
5 mg
¥ 833
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10 mg
¥ 1,130
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25 mg
¥ 1,780
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50 mg
¥ 2,410
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100 mg
¥ 3,190
现货
1 mL x 10 mM (in DMSO)
¥ 648
现货
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纯度: 99.65%
颜色: 白色
性状: Solid
资源下载: COA LCMS HNMR产品操作手册

产品介绍


GATA4-NKX2-5-IN-1 AI Summary
GATA4-NKX2-5-IN-1 inhibits the binding to the human growth hormone secretagogue receptor with an IC50 value of 8200.0 nM and the ghrelin-induced increase of intracellular [Ca2+] in CHO K cells with an IC50 value of 7600.0 nM. It acts as an antagonist at multiple receptors, including human GHS-R, GPR109A, PTH2 receptor, and CB2 receptor, showing inhibition percentages between 58.5% and 91.8% at a 10 µM concentration. It exhibits inhibitory effects on mouse GATA4/NKX2-5 transcriptional synergy with an IC50 of 3000.0 nM in COS-1 cells, and affects the interaction of GATA4/NKX2-5 in neonatal rat ventricular cardiomyocytes, leading to decreased mRNA levels of BNP and ANP, with inhibition percentages ranging from 32.0% to 81.0% at 10 µM concentration. GATA4-NKX2-5-IN-1 also inhibits VEGFR2 and EGFR at 30 µM with inhibition percentages of 64.0% and 54.0%, respectively, and the binding of GATA4 to [32P]-double stranded oligonucleotide with an inhibition percentage of 29.0% at 50 µM concentration. Furthermore, it influences the transcriptional activity of mouse NKX2-5 and GATA4 individually, showing activities of 49.0% and 62.0%, respectively, and induces cytotoxic effects, reducing cell viability by more than 10% at certain concentrations..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression.GATA4-NKX2-5-IN-1  dose-dependently inhibits the GATA4–NKX2-5 transcriptional synergy with an IC50 of 3 μM.
靶点活性
GATA4–NKX2-5:3 μM
化学信息
分子量349.43
分子式C21H23N3O2
CAS No.544681-96-1
SmilesC(NC1=CC=C(N(CC)CC)C=C1)(=O)C=2C(=NOC2C)C3=CC=CC=C3
密度1.176 g/cm3 (Predicted)
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.

实际储存温度请以COA为准

溶解度信息
DMSO: 65 mg/mL (186.02 mM), Sonication is recommended.
体内实验配方
10% DMSO+90% Corn Oil: 2.5 mg/mL (7.15 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
1mg5mg10mg50mg
1 mM2.8618 mL14.3090 mL28.6180 mL143.0902 mL
5 mM0.5724 mL2.8618 mL5.7236 mL28.6180 mL
10 mM0.2862 mL1.4309 mL2.8618 mL14.3090 mL
20 mM0.1431 mL0.7155 mL1.4309 mL7.1545 mL
50 mM0.0572 mL0.2862 mL0.5724 mL2.8618 mL
100 mM0.0286 mL0.1431 mL0.2862 mL1.4309 mL
该溶液配制表仅适用于固体产品。对于液体产品,请根据标明的浓度或密度计算稀释方案。

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:
比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL, 一共给药动物10只,您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH2O, 那么您的工作液浓度为2 mg/mL
母液配置方法:2 mg 药物溶于 100 μL DMSO ( 母液浓度为 20 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:100 μL DMSO 母液, 添加 400 μL PEG300 混匀澄清, 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 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: DMSOPEG300PEG400Tween 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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