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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
239440-20-1
- 规格:
1 mg/5 mg
| 规格: | 1 mg | 产品价格: | ¥4250.0 |
|---|---|---|---|
| 规格: | 5 mg | 产品价格: | ¥8500.0 |
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FR183998 free base
CAS No. : 239440-20-1
MCE 国际站:FR183998 free base
产品活性: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。
研究领域:Membrane Transporter/Ion Channel
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.
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. 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.
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