Ulipristal 是性孕酮受体 (Progesterone Receptor) 的选择性调节剂。它能够与孕激素受体结合,抑制 PR 介导的基因表达,降低生殖系统中孕激素的活性。
产品描述
Ulipristal is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure.
体外活性
Ulipristal acetate has partial agonistic as well as antagonistic effects on the progesterone receptor. It also binds to theglucocorticoid receptor, but has no relevant affinity to the estrogen, androgen and mineralocorticoid receptors.[1]
体内活性
Based on clinical trials, ulipristal acetate seems to be a reasonably tolerable and effective method of emergency contraception when used within 120 hours of intercourse. Ulipristal acetate is at least as effective as LNG when used within the first 72 hours after unprotected intercourse. However, ulipristal acetate may be more effective than LNG when used between 72 to 120 hours after unprotected intercourse, extending the window of opportunity for emergency contraception. [2][3]
Cas No.
159811-51-5
分子式
C28H35NO3
分子量
433.592
储存和溶解度
H2O:<1 mgml
DMSO:77 mg/mL (177.6 mM)
Ethanol:12 mg/mL (27.7 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years