生物活性
Hyperforin is the active ingredient in St. John′s Wort. It is used to treat depression, known to indirectly inhibit reuptake of serotonin and norepinephrine at the synapse, and recently discovered to exert its actions by directly activating TRPC6. TRPC6 is a member of the canonical transient receptor potential (TRPC) family of ion channels. DAG is the endogenous activator of this channel, and Hyperforin is the only known TRPC6-selective activator. Although it is broadly used, Hyperforin is chemically unstable. Efforts to find a stable but pharmacologically similar TRPC6 activator resulted in the discovery of Hyp9, a simplified phloroglucinol derivative. Like Hyperforin, Hyp9 inhibits serotonin reuptake and induces neurite outgrowth. It increases calcium entry into the cell and selectively increases current through TRPC6 channels.
化学数据
分子量 | 322.4 |
分子式 | C18H26O5 |
CAS号 | 3118-34-1 |
纯度 | >98% |
溶解性(25°C) | DMSO: ≥20 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 |
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 | 3.1017 mL | 15.5087 mL | 31.0174 mL |
5 mM | 0.6203 mL | 3.1017 mL | 6.2035 mL |
10 mM | 0.3102 mL | 1.5509 mL | 3.1017 mL |