| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 10g |
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Purity: ≥98%
Mifepristone (formerly RU-486; C-1073; RU-38486; Mifegyne; Pictovir; Mifepristonum; Mifepristona; Mifeprex; Corlux) is a synthetic steroid compound that has been approved as a medication used in combination with misoprostol to bring about an abortion during pregnancy. It is a highly active antagonist of progesterone receptor and glucocorticoid receptor with an IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone is used as used as an abortifacient in the first two months of pregnancy, and in smaller doses as an emergency contraceptive. As a contraceptive agent, Mifepristone has been reported to reduce the size of uterine fibroids, and inhibit the growth of meningioma cells in vitro, in experimental animal models and in patients with inoperable meningiomas.
| ln Vitro |
Extensive research on more potent and selective antiprogestins was sparked by the discovery of mifepristone, the first competitive progesterone antagonist [1]. After four days of exposure to 10 μM mifepristone, which is near to plasma amounts that humans can achieve, cell growth was measured. NSC 119875 has a stronger antiproliferative effect on HeLa cells when coupled with mifepristone. The IC50 of NSC 119875 plus mifepristone (14.2 μM) in HeLa cells was less than that of NSC 119875 alone (34.2 μM), a roughly 2.5-fold difference. Mifepristone treatment caused NSC 119875 accumulation in HeLa cells to increase twofold above NSC 119875 alone, with a significant difference (p=0.009) from 0.79 to 1.52 μg/mg protein[2].
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| ln Vivo |
When NSC 119875 is used in isolation to treat cervical tumor xenograft animals, tumor development is inhibited in comparison to the control group. By the end of the research, the combination of NSC 119875 and Mifepristone at the doses employed resulted in an even more substantial (p<0.05) drop in tumor weight, with a fall of almost 50% when compared to the therapies alone[2]. A 4-day binge-like EtOH dosing regimen (3 to 5 g/kg/ig every 8 hours) is administered to adult male Sprague-Dawley rats in order to achieve peak blood EtOH levels (BELs) of less than 300 mg/dL. Animal subgroups are injected subcutaneously with Mifepristone (20 or 40 mg/kg in peanut oil). While pretreatment with Mifepristone (40 mg/kg) greatly lessens the severity of EtOH withdrawal, Mifepristone itself does not appreciably alter the behavior of animals that have never used EtOH. There is a noteworthy interaction between drug and food (F(5,55)=3.92, p<0.05), wherein mice treated with EtOH and given either vehicle or 20 mg/kg of Mifepristone exhibit considerably higher indications of EtOH withdrawal compared to animals treated with EtOH without EtOH. Significantly, and in a dose-dependent manner, therapy with 40 mg/kg of mifepristone lessens the severity of EtOH withdrawal[3].
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| References |
[1]. Jiang W, et al. New progesterone receptor antagonists: phosphorus-containing 11beta-aryl-substituted steroids. Bioorg Med Chem. 2006 Oct 1;14(19):6726-32.
[2]. Jurado R, et al. NSC 119875 cytotoxicity is increased by mifepristone in cervical carcinoma: an in vitro and in vivo study. Oncol Rep. 2009 Nov;22(5):1237-45. [3]. Sharrett-Field L, et al. Mifepristone Pretreatment Reduces Ethanol Withdrawal Severity In Vivo. Alcohol Clin Exp Res. 2013 Aug;37(8):1417-23. [4]. Yuehua You, et al. Progesterone Promotes Endothelial Nitric Oxide Synthase Expression Through Enhancing Nuclear Progesterone receptor-SP1 Formation. Am J Physiol Heart Circ Physiol. 2020 Jul 3 |
| Molecular Formula |
C29H35NO2
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| Molecular Weight |
429.59
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| CAS # |
84371-65-3
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| Related CAS # |
Mifepristone (Standard);84371-65-3;Mifepristone-d3;Mifepristone-13C,d3
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| SMILES |
O([H])[C@@]1(C#CC([H])([H])[H])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=C3[C@@]([H])(C3C([H])=C([H])C(=C([H])C=3[H])N(C([H])([H])[H])C([H])([H])[H])C([H])([H])[C@@]21C([H])([H])[H])=O
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| InChi Key |
VKHAHZOOUSRJNA-GCNJZUOMSA-N
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| InChi Code |
InChI=1S/C29H35NO2/c1-5-15-29(32)16-14-26-24-12-8-20-17-22(31)11-13-23(20)27(24)25(18-28(26,29)2)19-6-9-21(10-7-19)30(3)4/h6-7,9-10,17,24-26,32H,8,11-14,16,18H2,1-4H3/t24-,25+,26-,28-,29-/m0/s1
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| Chemical Name |
(8S,11R,13S,14S,17S)-11-(4-(dimethylamino)phenyl)-17-hydroxy-13-methyl-17-(prop-1-yn-1-yl)-6,7,8,11,12,13,14,15,16,17-decahydro-1H-cyclopenta[a]phenanthren-3(2H)-one
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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 (5.82 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 (5.82 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 (5.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10 mg/mL (23.28 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3278 mL | 11.6390 mL | 23.2780 mL | |
| 5 mM | 0.4656 mL | 2.3278 mL | 4.6556 mL | |
| 10 mM | 0.2328 mL | 1.1639 mL | 2.3278 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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