生物活性
Ketanserin (Vulketan Gel) is specific 5-HT2A serotonin receptor antagonist with a Ki of 2.5 nM for rat and human 5-HT2A. Ketanserin (Vulketan Gel) is a drug with affinity for multiple G protein-coupled receptors. Ketanserin ( Vulketan Gel) inhibits rat and human 5-HT2C with Ki of 50 and100 nM, respectively and has higher affinity binding for alpha-1 adrenergic (Ki = ~ 40 nM) and Histamine H1 (Ki = 2 nM). Ketanserin (Vulketan Gel) can also be used to discriminate between 5-HT1D and 5-HT1B receptor subtypes. Ketanserin (Vulketan Gel) has antihypertensive properties. Ketanserin (Vulketan Gel) also reduces platelet aggregation produced by serotonin. Ketanserin also has high affinity for alpha-1 adrenergic receptors, and very high affinity for histamine H1 receptors. Ketanserin (Vulketan Gel) was shown to reduce the severity and frequency of the vasospasm in Raynaud’s phenomenon.
化学数据
分子量 | 395.43 |
分子式 | C22H22FN3O3 |
CAS号 | 74050-98-9 |
纯度 | >98% |
溶解性(25°C) | DMSO |
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 | 2.5289 mL | 12.6445 mL | 25.2889 mL |
5 mM | 0.5058 mL | 2.5289 mL | 5.0578 mL |
10 mM | 0.2529 mL | 1.2644 mL | 2.5289 mL |