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133804-44-1

中文名稱 133804-44-1
英文名稱 5-METHYL-2-(1-PIPERAZINYL)BENZENESULFONIC ACID MONOHYDRATE
CAS 133804-44-1
分子式 C11H16N2O3S
分子量 256.32
MOL 文件 133804-44-1.mol
133804-44-1 結構式 133804-44-1 結構式

基本信息

中文別名
化合物 T14857
英文別名
Caldaret
Benzenesulfonic acid, 5-methyl-2-(1-piperazinyl)-
5-METHYL-2-(1-PIPERAZINYL)BENZENESULFONIC ACID MONOHYDRATE

物理化學性質

密度1.302±0.06 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(pKa)-1.76±0.42(Predicted)
形態(tài)Solid
顏色White to light yellow

安全數據

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335

常見問題列表

生物活性
Caldaret 是一種細胞內 Ca2+ 調節(jié)劑,通過反向模式抑制 Na+/Ca2+ 交換作用。
靶點

Na + /Ca 2+ exchanger

體外研究

Caldaret (MCC-135) is demonstrated to restore Ca 2+ -ATPase activity of the sarcoplasmic reticulum (SR) isolated from the myocardium acutely exposed to ischemia and reperfusion in vitro.

體內研究

Caldaret, an intracellular Ca 2+ handling modulator, limits infarct size of reperfused canine heart. The cardioprotective effect of Caldaret, a novel intracellular Ca 2+ handling modulator that acts through reverse-mode Na + /Ca 2+ exchanger inhibition and potential sarcoplasmic reticulum (SR) Ca 2+ uptake enhancement, against reperfusion injury is investigated. Intravenously infused Caldaret (3 or 30 microg/kg per hour) for 30 min at left circumflex (LCX)-reperfusion markedly reduces infarct size (by 51.3% or 71.9%, respectively). The amelioration of intracellular Ca 2+ handling dysfunction achieved by Caldaret leads to cardioprotective effects against reperfusion injury following prolonged ischemia. Caldaret (MCC-135) is a new potent compound with beneficial effects in heart failure. In diabetic rats, Caldaret decreases TR80 significantly without significant effect on developed tension (DT). Caldaret has minimal effects on SR Ca 2+ uptake in normal rats, that is observed as increased SR Ca 2+ uptake at uptake time of 20 and 30 s at the highest concentration of 10 μM. In diabetic rats, Caldaret increases SR Ca 2+ uptake all over the range of uptake time. Both initial rate of SR Ca 2+ uptake and the amount of Ca 2+ accumulated in the SR with longer uptake time are increased by Caldaret.

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