生物活性
Tazarotene is a member of the acetylenic class of retinoids which binds at retinoid acid receptors (RAR) -β and -γ. Tazarotene is a retinoic acid receptor-specific retinoid with demonstrated efficacy in the topical treatment of psoriasis. Tazarotene exerts anti-inflammatory and immune-modulating activities toward both infective agents and damaged keratinocytes. Tazarotene down-regulates markers of keratinocyte differentiation, keratinocyte proliferation, and inflammation. It is also up-regulates three novel genes TIG-1 (tazarotene-induced gene-1), TIG-2, and TIG-3, which may mediate an antiproliferative effect.
化学数据
分子量 |
351.46 |
分子式 |
C21H21NO2S |
CAS号 |
118292-40-3 |
纯度 |
>99% |
溶解性(25°C) |
DMSO >30 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
以下数据基于半岛bd体育手机客户端 分子量,对于特殊半岛bd体育手机客户端 ,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 |
2.8453 mL |
14.2264 mL |
28.4527 mL |
5 mM |
0.5691 mL |
2.8453 mL |
5.6905 mL |
10 mM |
0.2845 mL |
1.4226 mL |
2.8453 mL |