4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is an orally active, selective estrogen receptor modulator (SERM).
IC50&Target
Estrogen receptor
3.3 nM (IC50)
CRISPR/Cas9
体外研究
4-Hydroxytamoxifen (Monohydroxytamoxifen) is a selective ostrogen receptor antagonist, with an IC50 of 3.3 nM for the [H]oestradiol binding to oestrogen receptor. 4-Hydroxytamoxifen (10, 100 nM) enables to inhibit the binding of [H]oestradiol to the human 8 S oestrogen receptor. 4-Hydroxytamoxifen activates intein-linked inactive Cas9, reduces off-target CRISPR-mediated gene editing. In human cells, conditionally active Cas9s modify target genomic sites with up to 25-fold higher specificity than wild-type Cas9.
体内研究
4-Hydroxytamoxifen (0.2, 1 and 5 μg/day, p.o.) causes a dose-related decrease in uterine wet weight of immature rats. 4-Hydroxytamoxifen (6 μg/0.1 mL sesame oil/day, s.c.) effectively attenuates methamphetamine-induced nigrostriatal dopamine depletions in bothsexes of intact and gonadectomized C57BL/6 J mice. 4-Hydroxytamoxifen does not alter the dopamine content levels in the striatum.
分子式
C26H29NO2
分子量
387.51
CAS号
68047-06-3
中文名称
4-羟基他莫昔芬
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 50 mg/mL (129.03 mM; ultrasonic and warming and heat to 60°C)