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Gestrinone (R 2323) Sale

(Synonyms: 孕三烯酮; R 2323) 目录号 : GC31746

An androgen and progesterone receptor ligand used to treat endometriosis

Gestrinone (R 2323) Chemical Structure

Cas No.:16320-04-0

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5mg
¥536.00
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10mg
¥803.00
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Sample solution is provided at 25 µL, 10mM.

Description

Endometriosis is common disease characterized by the presence of endometrial tissue outside the uterus which affects approximately 10% of premenopausal women. Gestrinone is a synthetic steroid used occasionally to treat endometriosis.1 It acts centrally on the hypothalamic-pituitary system to suppress release of lutenizing hormone (LH) and follicle-stimulating hormone (FSH), thus reducing estrogen synthesis.1 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.2 Gestrinone binds to AR and PR with EC50 values of approximately 20 and 30 nM, respectively.3 These values reflect approximately 5-6 fold lower affinity than testosterone and progesterone, the natural AR and PR ligands, for these receptors.3

1.Moghissi, K.S.Medical treatment of endometriosisClin. Obstet. Gynecol.45(3)620-633(1999) 2.Tamaya, T., Fujimoto, J., Watanabe, Y., et al.Gestrinone (R2323) binding to steroid receptors in human uterine endometrial cytosolActa Obstet. Gynecol. Scand.65(5)439-441(1986) 3.Death, A.K., mcGrath, K.C.Y., Kazluskas, R., et al.Tetrahydrogestrinone is a potent androgen and progestinJ. Clin. Endocrinol. Metab.89(5)2498-2500(2004)

实验参考方法

Cell experiment:

Gestrinone is dissolved in DMSO and diluted in cell culture media. The final concentration of DMSO in the culture media is 0.5%. The cells are cultured in 96-well plates and treated with DMSO or graded concentrations of gestrinone (0.1, 0.5, 1.0, 5.0, 10, 50 or 100 μM) for 20, 40 and 60 h. The absorbance (OD) at 450 nm is read to determine the cell viability in each well[2].

References:

[1]. Tamaya T, et al. Gestrinone (R2323) binding to steroid receptors in human uterine endometrial cytosol. Acta Obstet Gynecol Scand. 1986;65(5):439-41.
[2]. Zhu Y, et al. Gestrinone inhibits growth of human uterine leiomyoma may relate to activity regulation of ERα, Src and P38 MAPK. Biomed Pharmacother. 2012 Dec;66(8):569-77.
[3]. Snyder BW, et al. Studies on the mechanism of action of danazol and gestrinone (R2323) in the rat: evidence for a masked estrogen component. Fertil Steril. 1989 Apr;51(4):705-10.
[4]. Dowsett M, et al. A comparison of the effects of danazol and gestrinone on testosterone binding to sex hormone binding globulin in vitro and in vivo. Clin Endocrinol (Oxf). 1986 May;24(5):555-63.

化学性质

Cas No. 16320-04-0 SDF
别名 孕三烯酮; R 2323
Canonical SMILES C#C[C@]1(O)CC[C@@]2([H])[C@]3([H])CCC4=CC(CCC4=C3C=C[C@]12CC)=O
分子式 C21H24O2 分子量 308.41
溶解度 DMSO : ≥ 50 mg/mL (162.12 mM) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 3.2424 mL 16.2122 mL 32.4244 mL
5 mM 0.6485 mL 3.2424 mL 6.4849 mL
10 mM 0.3242 mL 1.6212 mL 3.2424 mL
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