Dienogest Inhibitor CAS No. 65928-58-7

Cat. No.	Name	Size	Price
KI1023	Dienogest	10 mg	$192
	Dienogest	25 mg	$432
	Dienogest	100 mg	$1232

Chemical Characteristic

Product Name	Dienogest
CAS No.	65928-58-7
Molecular Weight	311.42
Formula	C₂₀H₂₅NO₂
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
Smiles	C1(=O)CCC2=C3[C@@H](CCC2=C1)[C@@H]1CC[C@@](CC#N)([C@@]1(C)CC3)O
Chemical Structure

Biological activities

Dienogest is a orally-active semisynthetic, steroidal progestogen. Dienogest is also a 5 alpha-reductase inhibitor. The IC50 of dienogest is 55 µM against 5 alpha-reductase.^[1] In addition, dienogest is used as a selective progesterone receptor agonist. Dienogest activate progesterone receptor with an EC50 of 3.4 nM. Dienogest antagonizes androgen receptor with an EC50 of 421 nM.^[2] Dienogest exhibits endometrial activity with an ED50 of 4.2 µg/kg.^[2] Dienogest at the dose of 2 mg daily effectively alleviates the painful symptoms of endometriosis, reduces endometriotic lesions. ^[3] Dienogest (0.1-1 mg/kg per day, p.o.) decreases the endometrial implant volume Simultaneously, dienogest improves the endometrial implant-induced alterations of the immune system. Dienogest increases the natural killer activity of peritoneal fluid cells and splenic cells. Dienogest decreases the number of peritoneal fluid cells. Dienogest reduces interleukin-1beta generation by peritoneal macrophages.^[4]

References

[1] Rabe T, et al. Inhibition of skin 5 alpha-reductase by oral contraceptive progestins in vitro. Gynecol Endocrinol. 2000, 14(4): 223-230. [2] Sasagawa S, et al. Dienogest is a selective progesterone receptor agonist in transactivation analysis with potent oral endometrial activity due to its efficient pharmacokinetic profile. Steroids. 2008, 73(2): 222-231. [3] Schindler AE. Dienogest in long-term treatment of endometriosis. Int J Womens Health. 2011, 3: 175-184. [4] Katsuki Y, et al. Effects of dienogest, a synthetic steroid, on experimental endometriosis in rats. Eur J Endocrinol. 1998, 138(2): 216-226.

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