Dienogest

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Dienogest (STS-557) 一种口服有效的和具有选择性的孕酮受体激动剂，能有效减少 COX-2、mPGES-1 和芳香化酶的基因表达。Dienogest 还能抑制 PGE2 合成酶的 mRNA 和蛋白表达，以及 NF-κB 的激活。Dienogest 可用于子宫内膜异位症，更年期和月经过多的研究。

Dienogest is an orally active synthetic progesterone, used for contraception and the treatment of endometriosis.

Cell Viability Assay Cell Line:EM-PR cells Concentration:0.01-1 μM Incubation Time:24 h Result:Inhibited PGE2 production and suppressed NF-κB binding activity in the spheroid culture. Cell Viability Assay Cell Line:EM-PR cells Concentration:0.1 μM Incubation Time:24 h Result:Decreased the mRNA expression of the PGE2 synthases COX-2 and mPGES-1 compared with the respective control.Inhibited aromatase mRNA expression and increased the expression of COUP-TFII mRNA level.

Animal Model:Female Wistar rats (8 to 10-week-old; 180-220 g; rat endometrial autograft model).Dosage:1 mg/kg Administration:Oral administration; once daily for 14 days.Result:Showed significant suppression of angiogenesis of endometrial autografts, as indicated by the reduced size of the microvascular network and decreased microvessel density.Significantly reduced the level of perivascular α-smooth muscle actin within endometrial grafts.

STS 557

Endocrinology/Hormones

Estrogen Receptor/ERR

ER

Endocrinology

——

65928-58-7

311.42

C20H25NO2

>98% (HPLC)

DMSO: 62 mg/mL (199.08 mM)

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

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

(-20℃)

With Ice Pack

≥ 2 years