Gestrinone

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

孕三酮是一种合成的雄激素受体激动剂以及 ER 和孕激素受体拮抗剂，用于治疗子宫内膜异位症。它抑制平滑肌瘤细胞，IC50 为 43.67 μM。

Gestrinone is a synthetic androgen receptor agonist and ER and progesterone receptor antagonist used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.(In Vitro):Gestrinone binds to endometrial receptors for estrogen, progesterone and androgen, occupies all specific binding sites of steroids in the steroid target cells despite the presence of endogenous steroids. Gestrinone exhibits stronger inhibitory effects on the growth of leiomyoma cells at 60 h than that at 20 and 40 h. Leiomyoma cells appears less dense, the cytoplasm is atrophic, the intercellular connections dwindled and nuclear aggregations are observed with more than 10 μM gestrinone treatment. Gestrinone treatment reduces the relative mRNA levels of estrogen α in a concentration dependent manner at concentrations of 0.1-3.0 μM.(In Vivo):The estrogen-sensitive endpoints, vaginal keratinization and uterine progesterone receptor concentration, are enhanced by treatment with a combination of flutamide and either danazol or gestrinone. These data indicate that danazol and gestrinone have estrogenic activity that is masked by the androgenic component of these drugs. The mean hormone binding globulin treated with gestrinone fell from 56.4 nM to 28.1 nM after one week’s treatment and to 7.1 nM after 4 weeks respectively.

Gestrinone binds to endometrial receptors for estrogen, progesterone and androgen, occupies all specific binding sites of steroids in the steroid target cells despite the presence of endogenous steroids. Gestrinone exhibits stronger inhibitory effects on the growth of leiomyoma cells at 60 h than that at 20 and 40 h. Leiomyoma cells appears less dense, the cytoplasm is atrophic, the intercellular connections dwindled and nuclear aggregations are observed with more than 10 μM gestrinone treatment. Gestrinone treatment reduces the relative mRNA levels of estrogen α in a concentration dependent manner at concentrations of 0.1-3.0 μM.

The estrogen-sensitive endpoints, vaginal keratinization and uterine progesterone receptor concentration, are enhanced by treatment with a combination of flutamide and either danazol or gestrinone. These data indicate that danazol and gestrinone have estrogenic activity that is masked by the androgenic component of these drugs. The mean hormone binding globulin treated with gestrinone fell from 56.4 nM to 28.1 nM after one week’s treatment and to 7.1 nM after 4 weeks respectively.

R 2323

Endocrinology/Hormones

Estrogen Receptor/ERR

ER

Others

Endometriosis with or without accompanying sterility

16320-04-0

308.41

C21H24O2

>98% (HPLC)

DMSO:50 mg/mL (162.12 mM)

[H][C@@]12CC[C@@](O)(C#C)[C@@]1(CC)C=CC1=C3CCC(=O)C=C3CC[C@@]21[H]

(8S13S14S17S)-13-ethyl-17-ethynyl-17-hydroxy-126781314151617-decahydro-3H-cyclopenta[a]phenanthren-3-one

(-20℃)

With Ice Pack

≥ 2 years