生物活性
ST034307 is a selective inhibitor of adenylyl cyclase 1 (AC1) with analgesic activity. Adenylyl cyclase 1 has been shown to be a potential target for treating pain and reducing the dependency on opioids, but it has been difficult to inhibit AC1 selectively without also inhibiting other isoforms vital to physiological functions. ST034307 is selective for AC1 over all eight other adenylyl cyclase isoforms. It inhibited AC1 and reduced cAMP, while leaving AC8 unaffected and was shown to reduce pain in a mouse inflammatory pain model.
化学数据
分子量 | 297.95 |
分子式 | C10H4Cl4O2 |
CAS号 | 133406-29-8 |
纯度 | >98% |
溶解性(25°C) | DMSO: 2 mg/mL clear (warmed) |
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 |
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 | 3.3563 mL | 16.7813 mL | 33.5627 mL |
5 mM | 0.6713 mL | 3.3563 mL | 6.7125 mL |
10 mM | 0.3356 mL | 1.6781 mL | 3.3563 mL |