CAS NO: | 1803003-68-0 |
RN-9893 is a potent and selective antagonist of the Transient Receptor Potential ion channel TRPV4. RN-9893 has IC50values of 420 nM, 660 nM, and 320 nM for human, rat and mouse TRPV4 receptors, respectively. RN-9893 shows excellent selectivity over related TRP receptors with no inhibition of TRPV1 at a concentration of 10 μM, an IC50>30 μM against TRPV3, an IC50of approximately 30 μM against TRPM8, and also good selectivity using 54 binding assays against common biological targets.
分子量 | 500.49 |
分子式 | C21H23F3N4O5S |
CAS号 | 1803003-68-0 |
纯度 | >98% |
溶解性(25°C) | DMSO: 25 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 | 1.998 mL | 9.9902 mL | 19.9804 mL |
5 mM | 0.3996 mL | 1.998 mL | 3.9961 mL |
10 mM | 0.1998 mL | 0.999 mL | 1.998 mL |