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Gestrinone

13-ethyl-17α-hydroxy-18,19-dinorpregna-4,9,11-trien-20-yn-3-one

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货号 abs42018978
规格 价格
¥1820
库存状态:缺货
¥6160
库存状态:缺货

数量:

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概述
描述 Gestrinone is a synthetic steroid occasionally used to treat endometriosis. The common disease endometriosis is characterized by the presence of endometrial tissue outside the uterus which affects approximately 10% of premenopausal women. It acts centrally on the hypothalamic-pituitary system to suppress release of lutenizing hormone (LH) and follicle-stimulating hormone (FSH), thus reducing estrogen synthesis. It also binds to androgen (AR), progesterone (PR), and estrogen (ER) receptors in the human endometrial tissue but not to steroid hormone binding globulin or corticord-binding globulin. Gestrinone binds to AR and PR with EC50 values of approximately 20 and 30 nM, respectively. These values reflect approximately 5-6 fold lower affinity than testosterone and progesterone, the natural AR and PR ligands, for these receptors.
别名 13-ethyl-17α-hydroxy-18,19-dinorpregna-4,9,11-trien-20-yn-3-one
应用 A synthetic steroid that acts centrally on the hypothalamic-pituitary system
性能
密度 ~1.2 g/cm3 (Predicted)
熔点 150-152° C
沸点 ~507.6° C at 760 mmHg (Predicted)
保存方法 Store at -20° C
纯度 ≥99%
分子量 308.4
化学式 C21H24O2
溶解性 Soluble in ethanol (~20 mg/ml), DMSO (~20 mg/ml), DMF (~20 mg/ml), methanol, and water (0.25 mg/ml at 25° C).
CAS号 16320-04-0
折射率 n20D 1.61 (Predicted)
光学活性 α20/D +82.3°, c = 0.4 in methanol
IC50 Bind to AR: EC5050 ~20 nM; Bind to PR: EC5050 ~30 nM
PK值 pKa: 12.76 (Predicted), 17.88 (Predicted), pKb: -1.5 (Predicted)
SMILES CC[C@]12C=CC3=C4CCC(=O)C=C4CC[C@H]3[C@@H]1CC[C@]2(C#C)O
MDL MFCD00865561