239440-20-1
基本信息
化合物FR183998
1,3-Benzenedicarboxamide, N1-(aminoiminomethyl)-5-(2,5-dichloro-3-thienyl)-N3-[2-(dimethylamino)ethyl]-
物理化學(xué)性質(zhì)
報(bào)價(jià)日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價(jià)格 |
2024/11/08 | HY-100302 | 239440-20-1 FR183998 free base | 239440-20-1 | 1 mg | 1230元 |
2024/11/08 | HY-100302 | 239440-20-1 FR183998 free base | 239440-20-1 | 5 mg | 3150元 |
2024/11/08 | HY-100302 | 239440-20-1 FR183998 free base | 239440-20-1 | 10 mg | 4970元 |
常見問題列表
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)
FR183998 free base is a Na + /H + -exchange inhibitor, with IC 50 s of 0.3 nM, 6.5 nM and 3.1 nM by measurement of pH i change in rat lymphocytes, rat and human platelets, respectively.
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 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.