FR183998 free base
目录号: PL07617 纯度: ≥98%
CAS No. :239440-20-1
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中文名称
FR183998 free base
中文别名
化合物 T11319
英文名称
FR183998 free base
英文别名
FR183998 free base;1,3-Benzenedicarboxamide, N1-(aminoiminomethyl)-5-(2,5-dichloro-3-thienyl)-N3-[2-(dimethylamino)ethyl]-
Cas No.
239440-20-1
分子式
C17H19Cl2N5O2S
分子量
428.34
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
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。
生物活性
FR183998 free base is a potent Na/H-exchange inhibitor, with IC 50 s of 0.3 nM, 3.1 nM and 6.5 nM by measurement of pH i change in rat lymphocytes, rat and human platelets, respectively.
性状
Solid
IC50 & Target[1][2]
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)
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. 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 ED 50 s 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. 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 act
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
参考文献
[1]. Ohara F, et al. Preischemic and postischemic treatment with a new Na+/H+-exchange inhibitor, FR183998, shows cardioprotective effects in rats with cardiac ischemia and reperfusion. J Cardiovasc Pharmacol. 1999 Dec;34(6):848-56.
[2]. Ishizaki M, et al. Protective effect of FR183998, a Na+/H+ exchanger inhibitor, and its inhibition of iNOS induction in hepatic ischemia-reperfusion injury in rats. Shock. 2008 Sep;30(3):311-7.
溶解度数据
In Vitro: DMSO : 250 mg/mL (583.65 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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