1. Membrane Transporter/Ion Channel
  2. Na+/H+ Exchanger (NHE)
  3. FR183998 free base

FR183998 free base 

目录号: HY-100302 纯度: 98.00%
COA 产品使用指南

FR183998 free base 是一种有效的 Na+/H+-exchange 抑制剂,通过测量在大鼠淋巴细胞、血小板及人血小板 pHi 值的变化中,得到 IC50 值分别为 0.3 nM,6.5 nM 和 3.1 nM。

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FR183998 free base Chemical Structure

FR183998 free base Chemical Structure

CAS No. : 239440-20-1

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     可免费申领三个不同产品的试用装。

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1 mg ¥4250
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5 mg ¥8500
In-stock
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50 mg   询价  

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

FR183998 free base is a potent Na+/H+-exchange inhibitor, with IC50s of 0.3 nM, 3.1 nM and 6.5 nM by measurement of pHi change in rat lymphocytes, rat and human platelets, respectively.

IC50 & Target

IC50: 0.3 nM (Na+/H+-exchange, Rat lymphocytes), 3.1 nM (Na+/H+-exchange, Human platelet), 6.5 nM (Na+/H+-exchange, Rat platelet)[1]

体外研究
(In Vitro)

FR183998 free base is a Na+/H+-exchange inhibitor, with IC50s of 0.3 nM, 6.5 nM and 3.1 nM by measurement of pHi change in rat lymphocytes, rat and human platelets, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

FR183998 (0.1 and 1.0 mg/kg, i.v.) shows no effect hemodynamic parameters, and does not affect mean blood pressure and heart rate in conscious rats. Pretreatment of 0.01, 0.032, 0.10 mg/kg FR183998 or posttreament of 0.032 and 0.10 mg/kg FR183998 via intravenous administration, dose-dependently reuces reperfusion-induced ventricular fibrillation (VF) and mortality in reperfusion-induced arrhythmias in anesthetized rats, with ED50s against VF of 0.015 mg/kg and 0.070 mg/kg, respectively. FR183998 also reduces myocardial infarct sizes, and suppresses the arrhythmias in anesthetized rats[1]. FR183998 (1 mg/kg, i.v.) reduces the increase in serum levels of alanine transaminase, aspartate transaminase, and lactate dehydrogenase induced by hepatic I/R, and prevents the incidences of hepatic necrosis, apoptosis, and neutrophil infiltration. FR183998 blocks the I/R-induced activation of the NF-κB, reduces induction of iNOS and inhibits the production of nitric oxide. FR183998 also decreases the expression of the iNOS gene antisense transcript in the liver of hepatic I/R rats[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

428.34

Formula

C17H19Cl2N5O2S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 250 mg/mL (583.65 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3346 mL 11.6730 mL 23.3459 mL
5 mM 0.4669 mL 2.3346 mL 4.6692 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Cell Assay
[1]

Intracellular pH of rats lymphocytes is measured at 37°C with a spectrofluorometer by using the ratio of the emission (530 nm) obtained at 490- and 440-nm excitation wavelengths. After addition of 10 μL of the BCECF- and acid-loaded cells to 460 μL of Na-free buffer with 5 μL of DMSO or FR183998, 25 μL of 2.0 M NaCl (final 100 mM) is applied to start the reaction. The pHi change of cells is measured for >2 min. The initial increase in pHi in response to the added NaCl is taken as an estimate of Na+/H+-exchange activity, and the inhibitory effect of the drug is evaluated as IC50 value. The BCECF fluorescence signals are calibrated by titration with stepwise addition of small volumes of 1 M MES after permeabilization of the cells with 0.5% Triton X-100[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Male Sprague-Dawley rats age 9-10 weeks are anesthetized with sodium pentobarbital (50 mg/kg, i.p.), intubated, and ventilated with room air at a stroke volume of 4.5 mL with a frequency of 50 strokes/min. Saline or FR183998 is injected into the left femoral vein (bolus i.v.) 5 min before occlusion. Thoracotomy for coronary artery ligation is performed at the left side of the thorax above the heart, and the origin of the left anterior descending coronary artery is occluded by applying negative tension by aspiration through polyethylene tubing connected to the vacuum system, which can achieve regional ischemia. Successful occlusion is confirmed by ischemia-induced alteration of electrocardiogram (ECG). After 5-min ischemia, reperfusion is performed, and the incidence of ventricular tachycardia (VT) and ventricular fibrillation (VF) of >5 s is observed intermittently over a 5-min period of reperfusion[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3346 mL 11.6730 mL 23.3459 mL 58.3649 mL
5 mM 0.4669 mL 2.3346 mL 4.6692 mL 11.6730 mL
10 mM 0.2335 mL 1.1673 mL 2.3346 mL 5.8365 mL
15 mM 0.1556 mL 0.7782 mL 1.5564 mL 3.8910 mL
20 mM 0.1167 mL 0.5836 mL 1.1673 mL 2.9182 mL
25 mM 0.0934 mL 0.4669 mL 0.9338 mL 2.3346 mL
30 mM 0.0778 mL 0.3891 mL 0.7782 mL 1.9455 mL
40 mM 0.0584 mL 0.2918 mL 0.5836 mL 1.4591 mL
50 mM 0.0467 mL 0.2335 mL 0.4669 mL 1.1673 mL
60 mM 0.0389 mL 0.1945 mL 0.3891 mL 0.9727 mL
80 mM 0.0292 mL 0.1459 mL 0.2918 mL 0.7296 mL
100 mM 0.0233 mL 0.1167 mL 0.2335 mL 0.5836 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
FR183998 free base
目录号:
HY-100302
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