Gestrinone (R 2323)

目录号: GC31746纯度: >99.50%同义词: 孕三烯酮; R 2323

An androgen and progesterone receptor ligand used to treat endometriosis

Cas No.: 16320-04-0

规格	价格	库存	数量	操作
5mg	¥270.00	现货	1
10mg	¥432.00	现货	1

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618, 1017–1023 (2023)
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610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
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388(6745) (2025)
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387(6739) (2025)
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387(6734) (2025)
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产品描述 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 Experimental Reference Method

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.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号

16320-04-0

同义词

孕三烯酮; R 2323

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 g/mol

溶解性

DMSO : ≥ 50 mg/mL (162.12 mM)

保存条件

Store at -20°C

General tips

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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