Gestrinone-R-2323-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGestrinoneCat. No.: HY-101405CAS No.: 16320-04-0Synonyms: R 2323分式: CHO分量: 308.41作靶點(diǎn): Estrogen Receptor/ERR作通路: Others儲(chǔ)存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (162.12 mM)* means solub

2、le, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.2424 mL 16.2122 mL 32.4244 mL5 mM 0.6485 mL 3.2424 mL 6.4849 mL10 mM 0.3242 mL 1.6212 mL 3.2424 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天

3、使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.11 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (8.11 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Sma

4、ll Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (8.11 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Gestrinone (R2323)于治療宮內(nèi)膜異位癥的合成類(lèi)固醇激素。抑制平滑肌瘤的IC50值為43.67 M。IC50 & Target IC50: 43.67 M (leiomyoma cells) 2體外研究 Gestrinone binds to endometrial receptors for estrogen, progesterone and androgen, occupi

5、es all specificbinding sites of steroids in the steroid target cells despite the presence of endogenous steroids 1.Gestrinone exhibits stronger inhibitory effects on the growth of leiomyoma cells at 60 h than that at 20 and 40h. Leiomyoma cells appears less dense, the cytoplasm is atrophic, the inte

6、rcellular connections dwindled andnuclear aggregations are observed with more than 10 M gestrinone treatment. Gestrinone treatmentreduces the relative mRNA levels of estrogen in a concentration dependent manner at concentrations of0.1-3.0 M 2.體內(nèi)研究 The estrogen-sensitive endpoints, vaginal keratiniza

7、tion and uterine progesterone receptor concentration, areenhanced by treatment with a combination of flutamide and either danazol or gestrinone. These data indicatethat danazol and gestrinone have estrogenic activity that is masked by the androgenic component of thesedrugs 3. The mean hormone bindin

8、g globulin treated with gestrinone fell from 56.4 nM to 28.1 nM after oneweeks treatment and to 7.1 nM after 4 weeks respectively 4.PROTOCOLCell Assay 2 Gestrinone is dissolved in DMSO and diluted in cell culture media. The final concentration of DMSO in theculture media is 0.5%. The cells are cultu

9、red in 96-well plates and treated with DMSO or gradedconcentrations of gestrinone (0.1, 0.5, 1.0, 5.0, 10, 50 or 100 M) for 20, 40 and 60 h. The absorbance (OD)at 450 nm is read to determine the cell viability in each well 2.MCE has not independently confirmed the accuracy of these methods. They are

10、 for reference only.REFERENCES1. 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 ER, Src and

11、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 estrogencomponent. 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 vitroand in vivo. Clin Endocrinol (Oxf). 1986 May;24(5):555-63.McePdfHeight2/2 Master of Small Molecules 您邊的抑制劑師www.MedChemECaution: Product