CAS NO: | 133804-44-1 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
生物活性 | Caldaret is an intracellularCa2+handling modulator that acts through reverse modeNa+/Ca2+exchangerinhibition. | ||||||||||||||||
IC50& Target | Na+/Ca2+exchanger[1] | ||||||||||||||||
体外研究 (In Vitro) | Caldaret (MCC-135) is demonstrated to restore Ca2+-ATPase activity of the sarcoplasmic reticulum (SR) isolated from the myocardium acutely exposed to ischemia and reperfusion in vitro[2]. | ||||||||||||||||
体内研究 (In Vivo) | Caldaret, an intracellular Ca2+handling modulator, limits infarct size of reperfused canine heart. The cardioprotective effect of Caldaret, a novel intracellular Ca2+handling modulator that acts through reverse-mode Na+/Ca2+exchanger inhibition and potential sarcoplasmic reticulum (SR) Ca2+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 Ca2+handling dysfunction achieved by Caldaret leads to cardioprotective effects against reperfusion injury following prolonged ischemia[1]. 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 Ca2+uptake in normal rats, that is observed as increased SR Ca2+uptake at uptake time of 20 and 30 s at the highest concentration of 10 μM. In diabetic rats, Caldaret increases SR Ca2+uptake all over the range of uptake time. Both initial rate of SR Ca2+uptake and the amount of Ca2+accumulated in the SR with longer uptake time are increased by Caldaret[2]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 256.32 | ||||||||||||||||
Formula | C11H16N2O3S | ||||||||||||||||
CAS 号 | 133804-44-1 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 4.81 mg/mL(18.77 mM;ultrasonic and warming and adjust pH to 3 with HCl and heat to 60℃) 配制储备液
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