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239440-20-1

中文名稱 239440-20-1
英文名稱 FR183998 free base
CAS 239440-20-1
分子式 C17H19Cl2N5O2S
分子量 428.34
MOL 文件 239440-20-1.mol
239440-20-1 結(jié)構(gòu)式 239440-20-1 結(jié)構(gòu)式

基本信息

中文別名
化合物 T11319
化合物FR183998
英文別名
FR183998 free base
1,3-Benzenedicarboxamide, N1-(aminoiminomethyl)-5-(2,5-dichloro-3-thienyl)-N3-[2-(dimethylamino)ethyl]-

物理化學(xué)性質(zhì)

密度1.48±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)11.35±0.46(Predicted)
形態(tài)Solid
顏色White to off-white

安全數(shù)據(jù)

危險(xiǎn)性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
239440-20-1價(jià)格(試劑級)
報(bào)價(jià)日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價(jià)格
2024/11/08HY-100302239440-20-1
FR183998 free base
239440-20-11 mg1230元
2024/11/08HY-100302239440-20-1
FR183998 free base
239440-20-15 mg3150元
2024/11/08HY-100302239440-20-1
FR183998 free base
239440-20-110 mg4970元

常見問題列表

生物活性
FR183998 free base 是一種有效的 Na+/H+-exchange 抑制劑,通過測量在大鼠淋巴細(xì)胞、血小板及人血小板 pHi 值的變化中,得到 IC50 值分別為 0.3 nM,6.5 nM 和 3.1 nM。
靶點(diǎn)

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)

體外研究

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.

體內(nèi)研究

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.

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