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Dienogest(STS-557)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dienogest(STS-557)图片
CAS NO:65928-58-7
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)311.42
FormulaC20H25NO2
CAS No.65928-58-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 62 mg/mL (199.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other info

Chemical Name: 2-((8S,13S,14S,17R)-17-hydroxy-13-methyl-3-oxo-2,3,6,7,8,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl)acetonitrile

InChi Key: AZFLJNIPTRTECV-FUMNGEBKSA-N

InChi Code: InChI=1S/C20H25NO2/c1-19-8-6-16-15-5-3-14(22)12-13(15)2-4-17(16)18(19)7-9-20(19,23)10-11-21/h12,17-18,23H,2-10H2,1H3/t17-,18+,19+,20-/m1/s1

SMILES Code: N#CC[C@]1(O)CC[C@@]2([H])[C@]3([H])CCC4=CC(CCC4=C3CC[C@]12C)=O

SynonymsSTS-557; STS 557; STS557; BAY86-5258; BAY 86-5258; BAY-86-5258; Dinagest; Endometrion; M 18575; MJR-35; Visanne; ZK 37659.
实验参考方法
In Vitro

In vitro activity: Dienogest activates progesterone receptor (EC50=3.4 or 10.5 nM) with antagonistic activity on androgen receptor (EC50=420.6 or 775.0 nM) but not agonistic nor antagonistic action on GR, MR (3000 nM). Dienogest combined with Oestradiol leads to an increase in the levels of prolactin mRNA and prolactin production in a dose-dependent manner in human endometrial stromal cells (ESC). Dienogest directly acts on endometrial tissue in progestogenic response, such as decidualization, increases prolactin production and growth retardation. Dienogest at concentration of 0.1 μM and 1 μM significantly inhibits BrdU incorporation into DNA at 24 and 48 hours in the cultured endometriotic stromal cells. Dienogest significantly increases the cells in G0/G1 phase and reduces the cells in S phase and G2/M phase in 24 and 48 hours in the cultured endometriotic stromal cells.

In VivoDienogest (0.1-1 mg/kg per day, p.o.) reduces the endometrial implant volume to the same extent as Danazol (100 mg/kg per day, p.o.) in rats. Dienogest ameliorates the endometrial implant-induced alterations of the immune system: i.e. it increases the natural killer activity of peritoneal fluid cells and splenic cells, decreases the number of peritoneal fluid cells, and decreases interleukin-1beta production by peritoneal macrophages. Dienogest (0.1 mg/kg per day) combined with Buserelin (0.3 mg/kg per day) suppresses the bone mineral loss induced by buserelin alone, with no reduction of the effect on endometrial implants.
Animal modelRats
Formulation & Dosage0.1-1 mg/kg per day, p.o.
References

Steroids. 2008 Feb;73(2):222-31; Eur J Endocrinol. 1998 Feb;138(2):216-26.