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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENorethindrone acetateCat. No.: HY-B1710CAS No.: 51-98-9Synonyms: 19-Norethindrone acetate分式: CHO分量: 340.46作靶点: Progesterone Receptor作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO
2、: 100 mg/mL (293.72 mM)H2O : 0.67 mg/mL (1.97 mM; Need ultrasonic)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9372 mL 14.6860 mL 29.3720 mL5 mM 0.5874 mL 2.9372 mL 5.8744 mL10 mM 0.2937 mL 1.4686 mL 2.9372 mL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,并请注意储备液的保存式和期限
3、。体内实验请根据您的实验动物和给药式选择适当的溶解案,配制前请先配制澄清的储备液,再依次添加助溶剂(为保证实验结果的可靠性,体内实验的作液,建议您现现配,当天使;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占):1. 请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.34 mM); Clear solution2. 请依序添加每种溶剂: 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small
4、Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (7.34 mM); Clear solution3. 请依序添加每种溶剂: 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.34 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Norethindrone acetateFDA批准于治疗宫内膜异位症,由异常激素平引起的宫出症和继发性闭经的性孕激素。IC50 & Target Progesterone Receptor 1体内研究 Norethindrone ace
5、tate could be a cost-effective alternative with relatively mild side effects in the treatment ofsymptomatic endometriosis. Subjects treated with norethindrone acetate obtain dysmenorrhea and noncyclicpelvic pain relief 1. Norethindrone acetate alone is a well-tolerated, effective option to manage pa
6、in andbleeding for all stages of endometriosis. Post-Norethindrone acetate bleeding scores are improvedregardless of prior hormonal regimen, and post-Norethindrone acetate pain scores improved in all patientsexcept for those previously prescribed GnRH-agonist plus add-back 2. Norethindrone acetate s
7、hows lowacute toxicity in experimental animals and is consistent with the lack of toxicity seen in humans.Administration of norethindrone acetate alone to rodents at several multiples of the human dose results in notreatment related mortality, hematological changes, behavioral changes, or organ path
8、ology 3.Norethindrone acetate administration leads to significant and proportional reductions of the concentrations oftriglycerides, cholesterol and phospholipids of plasma lipoproteins of density 4.PROTOCOLAnimal Rats: Female Sprague-Dawley rats (200-210 g), 6 of which serve as controls, are indivi
9、dually caged in anAdministration 4 animal room illuminated from 9:00 a.m. to 9:00 p.m. Each of the 7 rats receiving norethindrone acetate is fed35 g/day for 2 weeks. Water and the rat chow which is high in carbohydrate are available ad libitum 4.MCE has not independently confirmed the accuracy of th
10、ese methods. They are for reference only.REFERENCES1. Muneyyirci-Delale O, et al. Effect of norethindrone acetate in the treatment of symptomatic endometriosis. Int J Fertil Womens Med.1998 Jan-Feb;43(1):24-7.2. Kaser DJ, et al. Use of norethindrone acetate alone for postoperative suppression of end
11、ometriosis symptoms. J Pediatr AdolescGynecol. 2012 Apr;25(2):105-8.3. Maier WE, et al. Pharmacology and toxicology of ethinyl estradiol and norethindrone acetate in experimental animals. Regul ToxicolPharmacol. 2001 Aug;34(1):53-61.4. Cheng DC, et al. Norethindrone acetate inhibition of triglyceride synthesis and release by rat hepatocytes. Atherosclerosis. 1983Jan;46(1):41-8.McePdfHeight2/2 Master of Small Molecules 您边的抑制剂师www.MedChemECaution: Product h
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