| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Asoprisnil targets the progesterone receptor (PR), a nuclear receptor that mediates the effects of the hormone progesterone. Progesterone plays a critical role in the growth and proliferation of uterine fibroids. Asoprisnil is a selective progesterone receptor modulator (SPRM), which means it can act as either an agonist or an antagonist depending on the tissue and the context. It exhibits mixed progesterone agonist and antagonist effects. By modulating PR activity, Asoprisnil inhibits the growth of uterine fibroids, which are progesterone-sensitive tumors.
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| ln Vitro |
In vitro, Asoprisnil has been shown to modulate progesterone receptor activity. It exhibits mixed progesterone agonist and antagonist effects on various progesterone-targeted tissues. Its activity is typically measured using cell-based reporter assays, where its ability to activate or inhibit PR-mediated transcription is assessed. The compound's effects on the proliferation of uterine fibroid cells can also be studied in vitro. However, specific in vitro data, such as IC50 or EC50 values, are not detailed in standard product descriptions.
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| ln Vivo |
In vivo, Asoprisnil has been studied in clinical trials for the treatment of uterine fibroids. Several Phase 2 and Phase 3 studies have been completed, evaluating its safety and effectiveness. The compound has been shown to reduce fibroid size and improve symptoms associated with uterine fibroids. However, specific in vivo efficacy data, such as detailed results from these trials, are not provided in standard product descriptions. Asoprisnil is a research compound that has been investigated for therapeutic use.
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| Enzyme Assay |
The in vitro assays for Asoprisnil measure its binding to the progesterone receptor and its ability to modulate PR-mediated transcription. Receptor binding assays are performed using the progesterone receptor and a radiolabeled ligand. Functional assays measure the compound's ability to activate or inhibit the transcription of a reporter gene under the control of a progesterone response element (PRE). Cells are transfected with the reporter construct and treated with Asoprisnil. The modulation of reporter gene expression is measured. These assays confirm that Asoprisnil is a selective progesterone receptor modulator.
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| Cell Assay |
In vitro cell-based assays for Asoprisnil are conducted using cells expressing the progesterone receptor, such as T47D breast cancer cells. In a typical assay, cells are transfected with a PRE-luciferase reporter plasmid and treated with Asoprisnil. Luciferase activity is measured to assess the compound's ability to modulate PR-mediated transcription. The compound's effects on cell proliferation can also be assessed. These cell-based assays confirm that Asoprisnil modulates PR activity.
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| Animal Protocol |
In vivo animal experiments for Asoprisnil are not detailed in standard product descriptions. As a compound that has been investigated in clinical trials for uterine fibroids, it would have been evaluated in animal models. In a typical study, rodents or other animals with hormone-induced uterine fibroids would be treated with Asoprisnil, and fibroid growth would be monitored. However, specific protocols for Asoprisnil are not provided in the available literature. Its use is limited to research applications and historical clinical studies.
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| ADME/Pharmacokinetics |
Asoprisnil has a molecular weight of 449.58 g/mol and a molecular formula of C28H35NO4. It has a purity of 98%. It is soluble in DMSO and other organic solvents. For storage, it is recommended to keep the powder at -20°C. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have been studied in the context of clinical development. However, specific values are not detailed in standard product descriptions.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for Asoprisnil is not provided in standard product descriptions. As a selective progesterone receptor modulator that has been investigated in clinical trials, its safety profile has been evaluated. Common side effects may include endometrial changes, which are a known effect of SPRMs. However, specific toxicity data, such as LD50 or organ toxicity, are not detailed. As with all research chemicals and pharmaceuticals, it should be handled with caution using appropriate safety measures.
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| References |
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| Additional Infomation |
Asoprisnil (J867) is a selective progesterone receptor modulator. It can be used to treat progesterone-sensitive uterine fibroids.
Drug Indications It has been studied for the treatment of uterine fibroids. Asoprisnil (J867) is a research compound and a pharmaceutical agent that has been investigated for the treatment of uterine fibroids. It is a selective progesterone receptor modulator (SPRM) that exhibits mixed progesterone agonist and antagonist effects. It has been studied in several Phase 2 and Phase 3 clinical trials for the treatment of uterine fibroids. However, it is not currently approved for clinical use in many countries. Asoprisnil is a valuable research tool for studying the role of progesterone in uterine fibroid growth and for exploring the therapeutic potential of SPRMs. |
| Molecular Formula |
C28H35NO4
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|---|---|
| Molecular Weight |
449.591
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| Exact Mass |
449.257
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| CAS # |
199396-76-4
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| PubChem CID |
9577221
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| Appearance |
White to off-white solid powder
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| Vapour Pressure |
0mmHg at 25°C
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| LogP |
5.425
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
33
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| Complexity |
867
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C[C@]12C[C@@H](C3=C4CCC(=O)C=C4CC[C@H]3[C@@H]1CC[C@]2(COC)OC)C5=CC=C(C=C5)/C=N/O
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| InChi Key |
GJMNAFGEUJBOCE-MEQIQULJSA-N
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| InChi Code |
InChI=1S/C28H35NO4/c1-27-15-24(19-6-4-18(5-7-19)16-29-31)26-22-11-9-21(30)14-20(22)8-10-23(26)25(27)12-13-28(27,33-3)17-32-2/h4-7,14,16,23-25,31H,8-13,15,17H2,1-3H3/b29-16+/t23-,24+,25-,27-,28+/m0/s1
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| Chemical Name |
(8S,11R,13S,14S,17S)-11-[4-[(E)-hydroxyiminomethyl]phenyl]-17-methoxy-17-(methoxymethyl)-13-methyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one
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| Synonyms |
J867 J 867 AsoprisnilumJ-867Asoprisnil
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2242 mL | 11.1212 mL | 22.2425 mL | |
| 5 mM | 0.4448 mL | 2.2242 mL | 4.4485 mL | |
| 10 mM | 0.2224 mL | 1.1121 mL | 2.2242 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00156156 | COMPLETED | Drug: Asoprisnil Drug: Asoprisnil |
Fibroid Uterus Leiomyoma Menorrhagia Metrorrhagia Uterine Fibroids |
Abbott | 2004-11 | Phase 3 |
| NCT00156208 | COMPLETED | Drug: Asoprisnil Drug: Asoprisnil |
Fibroid Uterus Leiomyoma Menorrhagia Metrorrhagia Uterine Fibroids |
Abbott | 2004-04 | Phase 3 |
| NCT00156195 | COMPLETED | Drug: Asoprisnil Drug: Asoprisnil |
Leiomyoma Menorrhagia Metrorrhagia |
Abbott | 2003-09 | Phase 3 |
| NCT00160459 | COMPLETED | Drug: Asoprisnil Drug: Asoprisnil Drug: Asoprisnil Drug: Placebo |
Leiomyoma | Abbott | 2000-05 | Phase 2 |
| NCT00160433 | COMPLETED | Drug: Asoprisnil Drug: Asoprisnil Drug: Asoprisnil Drug: Placebo |
Endometriosis | Abbott | 2002-08 | Phase 2 |
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