生物活性
KB-R7943 is a plasma membrane Na(+)/Ca(2+) exchanger inhibitor. KB-R7943 reversibly inhibits inward and outward Na+/Ca2+ exchange in a dose-dependent manner (MCU; IC50 = 5.5 μM), but it does not affect Na+-dependent transport systems or ionotropic glutamate receptors. In addition, the effects of KB-R7943 on Ca(2+) homeostasis provide new evidence for the role of mitochondria modulating Ca(2+)-release and regenerative Ca(2+)-oscillations. KB-R7943 (10 and 30 microM) suppressed the tonotropic effect of ouabain, and prolonged the onset time of extra-systole induced by ouabain in isolated atria. KB-R7943 suppresses ouabain-induced arrhythmias through inhibition of the reverse-mode NCX. KB-R7943 is also a potent blocker of the transient receptor potential channels (TRPC) TRPC3, TRPC5 and TRPC6.
化学数据
| 分子量 | 427.49 |
| 分子式 | C16H17N3O3S.CH3SO3H |
| CAS号 | 182004-65-5 |
| 纯度 | 99.48% |
| 溶解性（25°C） | DMSO 27 mg/mL |
| 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 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | neurons, astrocytes, and microglia |
| 方法 | Na+-Ca2+ Exchange Activity.
Na+-Ca2+ exchange activity was determined by assaying Na+-dependent Ca2+ uptake as reported previously (Takuma et al., 1994). Briefly, the cells were preincubated in Hanks' balanced saline solution (HBSS) for 20 min, and the medium was switched to HBSS containing Ca2+ and incubated for 5 min. To increase intracellular Na+ concentration, 1 mM ouabain plus 20 μM monensin (for astrocytes and microglia) and 10 μM monensin (for neurons) were used. Monensin was added simultaneously with the isotope. Ouabain was added 5 min before monensin in astrocytes and microglia. NCX inhibitors were added 5 min before monensin and present during Ca2+ uptake reaction. |
| 浓度 | 0~10 μ M |
| 处理时间 | 5 min |
| 动物实验 |
|---|
| 动物模型 | cerebral cortex (A) and striatum (B) after MCA occlusion in rats |
| 配制 | 20% soybean oil |
| 剂量 | 3 mg/kg |
| 给药处理 | bolus i.v. |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 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。
储备液配制
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 | 2.3392 mL | 11.6962 mL | 23.3924 mL |
| 5 mM | 0.4678 mL | 2.3392 mL | 4.6785 mL |
| 10 mM | 0.2339 mL | 1.1696 mL | 2.3392 mL |
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