| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Dienogest (formerly BAY86-5258; M-18575; MJR-35; ZK-37659; STS-557; Dinagest; Endometrion; Visanne) is a synthetic and orally bioavailable progesterone that was approved for use in contraception and 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.
| ln Vitro |
Dienogest (0.01-1 μM; 24 h) decreases PGE2 synthesis by inhibiting PGE2 synthase gene expression and simultaneously inhibits NF-κB activity in spheroid cultures [1]. Dienogest (0.1 μM; 24 h) suppresses the expression of aromatase expression genes and COUP-TFII mRNA in a PGE2-independent manner [1].
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| ln Vivo |
In a rat endometrial autotransplantation model, dienogest (1 mg/kg; orally once daily for 14 days) modulates angiogenesis in ectopic endometrial lesions [2].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: EM-PR cells Tested Concentrations: 0.01-1 µM Incubation Duration: 24 h Experimental Results: Inhibited PGE2 production and suppressed NF-κB binding activity in the spheroid culture. Cell Viability Assay[1] Cell Types: EM-PR cells Tested Concentrations: 0.1 µM Incubation Duration: 24 h Experimental Results: diminished 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 Protocol |
Animal/Disease Models: Female Wistar rats (8 to 10weeks old; 180-220 g; rat endometrial autograft model)[2].
Doses: 1 mg/kg Route of Administration: Oral administration; one time/day for 14 days. Experimental Results: demonstrated significant suppression of angiogenesis of endometrial autografts, as indicated by the decreased size of the microvascular network and diminished microvessel density. Dramatically decreased the level of perivascular α-smooth muscle actin within endometrial grafts. |
| References |
[1]. Shimizu Y, et al. Dienogest, a synthetic progestin, inhibits prostaglandin E2 production and aromatase expression by human endometrial epithelial cells in a spheroid culture system. Steroids. 2011 Jan;76(1-2):60-7.
[2]. Katayama H, et al. Effect of dienogest administration on angiogenesis and hemodynamics in a rat endometrial autograft model. Hum Reprod. 2010 Nov;25(11):2851-8. |
| Molecular Formula |
C20H25NO2
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| Molecular Weight |
311.42
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| CAS # |
65928-58-7
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| Related CAS # |
Dienogest-d4;Dienogest-d5;Dienogest-d6
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| SMILES |
O([H])[C@@]1(C([H])([H])C#N)C([H])([H])C([H])([H])[C@@]2([H])[C@]3([H])C([H])([H])C([H])([H])C4=C([H])C(C([H])([H])C([H])([H])C4=C3C([H])([H])C([H])([H])[C@@]21C([H])([H])[H])=O
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| InChi Key |
AZFLJNIPTRTECV-FUMNGEBKSA-N
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| 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
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| 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
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2111 mL | 16.0555 mL | 32.1110 mL | |
| 5 mM | 0.6422 mL | 3.2111 mL | 6.4222 mL | |
| 10 mM | 0.3211 mL | 1.6055 mL | 3.2111 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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