CAS NO: | 1802013-08-6 |
ITH12575 is apotent and selective inhibitor of mitochondrial Na+/Ca2+ exchanger mNCX with neuroprotective activity. It was shown to reduce Ca2+ efflux from the mitochondria to the cytosol with an EC50 value of 690 nM and was shown to protect against Ca2+ overload and mitigated the neuronal damage in a model of oxidative stress. At higher concentrations ITH12575 also reduced Ca2+ influx through CALHM1, a Ca2+ channel that plays a key role in the neuronal electrical activity.
分子量 | 331.86 |
分子式 | C18H18ClNOS |
CAS号 | 1802013-08-6 |
纯度 | >98% |
溶解性(25°C) | DMSO: 2 mg/mL clear |
储存和运输条件 | 固体粉末: -20°C 冷藏长期储存 常温运输及临时存放 |
小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 3.0133 mL | 15.0666 mL | 30.1332 mL |
5 mM | 0.6027 mL | 3.0133 mL | 6.0266 mL |
10 mM | 0.3013 mL | 1.5067 mL | 3.0133 mL |