货号:A198037
同义名:
地诺孕素
/ STS 557
Dienogest (STS-557) 是一种口服有效的选择性孕酮受体激动剂,能够下调 COX-2、mPGES-1 和芳香化酶的基因表达,同时抑制 PGE2 合成酶的 mRNA 和蛋白水平以及 NF-κB 的激活。该化合物常用于子宫内膜异位症、更年期相关变化及月经过多等的机制研究。


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| 靶点 |
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| 描述 | Dienogest is a specific progesterone receptor agonist with potent oral endometrial activity and is used in the treatment of endometriosis. It is available for use as an oral contraceptive in combination with ethinylestradiol. It has antiandrogenic activity and as a result can improve androgenic symptoms. It is a non-ethinylated progestin which is structurally related to testosterone[3]. Dienogest inhibits ovulation, produces secretory transformation of the endometrium and has antiproliferative effects. Oral dienogest 2 mg/day plus ethinylestradiol 30 micrograms/day provides effective contraception (Pearl Index approximately 0.2). Cycle stability is good during long term use of this combination; irregular vaginal bleeding was evident in 6% of women after 12 months' use. Androgenic symptoms (including hirsutism, seborrhoea, alopecia, acne vulgaris and hair and skin greasiness) improved in women treated with dienogest plus ethinylestradiol[4]. Dienogest 2 mg/day was superior to placebo in reducing pelvic pain, with similar results to buserelin, leuprorelin, leuprolide acetate and triptorelin, in controlling symptoms associated with endometriosis. Dienogest 2 mg/day was effective in reducing endometriotic lesions. The extended therapy with dienogest 2 mg/day also showed an improvement in pelvic pain after 24-52 weeks with tolerable side effects[5]. Dienogest 2 mg once daily is effective and safe in the long-term management of EAPP in Chinese women with endometriosis, with progressive decreases in EAPP (endometriosis-associated pelvic pain) and bleeding irregularities during continued treatment[6]. |
| Concentration | Treated Time | Description | References | |
| immortalized human uterine epithelial cells | 1 μM | 72 h | To evaluate the anti-proliferative effect of DNG on KRAS-mutated cells, results showed that KRAS mutations diminished the anti-proliferative effect of DNG | Nat Commun. 2019 Dec 19;10(1):5785 |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00280657 | Acne Vulgaris | Phase 3 | Completed | - | - |
| NCT00764881 | - | Completed | - | - | |
| NCT02636972 | - | Unknown | January 2016 | Australia, South Australia ... 展开 >> PARC, Royal Adelaide Hospital Adelaide, South Australia, Australia, 5000 收起 << | |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.21mL 0.64mL 0.32mL |
16.06mL 3.21mL 1.61mL |
32.11mL 6.42mL 3.21mL |
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| CAS号 | 65928-58-7 |
| 分子式 | C20H25NO2 |
| 分子量 | 311.42 |
| SMILES Code | C[C@@]12[C@@](CC#N)(O)CC[C@@]1([H])[C@]3([H])CCC4=CC(CCC4=C3CC2)=O |
| MDL No. | MFCD00868356 |
| 别名 | 地诺孕素 ;STS 557 |
| 运输 | 蓝冰 |
| InChI Key | AZFLJNIPTRTECV-FUMNGEBKSA-N |
| Pubchem ID | 68861 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 25 mg/mL(80.28 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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