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抑制剂描述:

产品名称:Ethynodiol diacetate

产品别名:见爱必信官网

英文别名:Ethynodiol diacetate

靶点:Progesterone Receptor

CAS:297-76-7

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Ethynodiol diacetate是第一批合成的避孕药用孕激素之一。去甲二氢愈创木酸(NDGA) (< 1.5 μM)在150 μg/mL ethynodiol diacetate处理的人淋巴细胞中可以降低姐妹染色单体的交换率(SCEs)。在S9混合物存在的情况下NDGA处理会减轻ethynodiol diacetate 引起的遗传毒性损伤,这可能是通过对细胞色素P450s的抑制实现的而P450s会阻止ethynodiol diacetate的代谢活化,也可能是由于 NDGA具有清除自由基的功能。在S9混合物存在的情况下, Ethynodiol diacetate (150 μg/mL)会增加人淋巴细胞中姐妹染色单体的交换率(SCEs)和染色体畸变(CAs)频率并能 抑制淋巴细胞增殖。

溶解性:DMSO :71 mg/mL (184.7 mM) Water :71 mg/mL (184.7 mM)

体外研究:

Nordihydroguaiaretic acid (NDGA) ( Ethynodiol diacetate (150 μg/mL) increases sister chromatid exchanges (SCEs) and chromosomal aberrations (CAs) frequencies and inhibits lymphocyte proliferation in the presence of S9 mix in human lymphocyte.

体内研究:Ethynodiol diacetate (6 mg/kg b.w. daily) significantly increases the amounts of excreted 3alpha-hydroxy-5alpha-pregnan-20-one and A-homo-3-oxa-5alpha-pregnane-4,20-dione in urine in female rats. Significant increase in the weights of pituitary, liver and kidneys are noted in rats treated with ethynodiol diacetate (6 mg/kg b.w. daily). Norgestrel (75 μg/day) and ethynodiol diacetate (150 μg/day), co-administered with ethinyl estradiol (7.5 μg/day), lowers the plasma concentrations of HDL cholesterol in cynomolgus monkeys.

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