Asoprisnil
Based on 1 Customer Validation
Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.30%
- CAS No.: 199396-76-4
- Formule: C28H35NO4
- Masse moléculaire:449.58
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
>100 nM
Compound: 1, J-867
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Agonist activity at human PRB expressed in CHO cells
Agonist activity at human PRB expressed in CHO cells
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[PMID: 18243712] |
| CHO | IC50 |
0.2 nM
Compound: 1, J-867
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Antagonist activity at human PRB expressed in CHO cells assessed as inhibition of Org 2058 induced-transactivation
Antagonist activity at human PRB expressed in CHO cells assessed as inhibition of Org 2058 induced-transactivation
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[PMID: 18243712] |
| COS-7 | IC50 |
1600 nM
Compound: 5, asoprisnil
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Antagonist activity at human MR ligand binding domain expressed in african green monkey COS7 cells in presence of aldosterone by Gal4 hybrid assay
Antagonist activity at human MR ligand binding domain expressed in african green monkey COS7 cells in presence of aldosterone by Gal4 hybrid assay
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[PMID: 18318463] |
| COS-7 | IC50 |
1900 nM
Compound: 5, asoprisnil
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Antagonist activity at human ER ligand binding domain expressed in african green monkey COS7 cells in presence of 17-beta-estradiol by Gal4 hybrid assay
Antagonist activity at human ER ligand binding domain expressed in african green monkey COS7 cells in presence of 17-beta-estradiol by Gal4 hybrid assay
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[PMID: 18318463] |
| COS-7 | IC50 |
6.1 nM
Compound: 5, asoprisnil
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Antagonist activity at human AR ligand binding domain expressed in african green monkey COS7 cells in presence of 5-alpha-dihydrotestosterone by Gal4 hybrid assay
Antagonist activity at human AR ligand binding domain expressed in african green monkey COS7 cells in presence of 5-alpha-dihydrotestosterone by Gal4 hybrid assay
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[PMID: 18318463] |
| COS-7 | IC50 |
85 nM
Compound: 5, asoprisnil
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Antagonist activity at human GR ligand binding domain expressed in african green monkey COS7 cells in presence of Dexamethasone by Gal4 hybrid assay
Antagonist activity at human GR ligand binding domain expressed in african green monkey COS7 cells in presence of Dexamethasone by Gal4 hybrid assay
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[PMID: 18318463] |
| T47D | IC50 |
0.3 nM
Compound: 2
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Antagonist activity against progesterone receptor in human T47D cells by alkaline phosphatase assay
Antagonist activity against progesterone receptor in human T47D cells by alkaline phosphatase assay
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[PMID: 23079530] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 199396-76-4
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Appearance Solid
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Masse moléculaire 449.58
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Formule C28H35NO4
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Color White to off-white
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SMILES
C[C@@]12[C@@](OC)(CC[C@]1([C@@]3(CCC4=CC(CCC4=C3[C@H](C2)C5=CC=C(C=C5)/C=N/O)=O)[H])[H])COC
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Synonyms
J867
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 45 mg/mL (100.09 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Stewart EA, et al. Safety and efficacy of the selective progesterone receptor modulator asoprisnil for heavy menstrual bleeding with uterine fibroids: pooled analysis of two 12-month, placebo-controlled, randomized trials. Hum Reprod. 2019 Apr 1;34(4):623 [Content Brief]
[2]. Wu XL, et al. Postcoital administration of asoprisnil inhibited embryo implantation and disturbed ultrastructure of endometrium in implantation window in mice. J Huazhong Univ Sci Technolog Med Sci. 2013 Apr;33(2):277-283. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2243 mL | 11.1215 mL | 22.2430 mL | 55.6075 mL |
| 5 mM | 0.4449 mL | 2.2243 mL | 4.4486 mL | 11.1215 mL | |
| 10 mM | 0.2224 mL | 1.1121 mL | 2.2243 mL | 5.5607 mL | |
| 15 mM | 0.1483 mL | 0.7414 mL | 1.4829 mL | 3.7072 mL | |
| 20 mM | 0.1112 mL | 0.5561 mL | 1.1121 mL | 2.7804 mL | |
| 25 mM | 0.0890 mL | 0.4449 mL | 0.8897 mL | 2.2243 mL | |
| 30 mM | 0.0741 mL | 0.3707 mL | 0.7414 mL | 1.8536 mL | |
| 40 mM | 0.0556 mL | 0.2780 mL | 0.5561 mL | 1.3902 mL | |
| 50 mM | 0.0445 mL | 0.2224 mL | 0.4449 mL | 1.1121 mL | |
| 60 mM | 0.0371 mL | 0.1854 mL | 0.3707 mL | 0.9268 mL | |
| 80 mM | 0.0278 mL | 0.1390 mL | 0.2780 mL | 0.6951 mL | |
| 100 mM | 0.0222 mL | 0.1112 mL | 0.2224 mL | 0.5561 mL |
Asoprisnil Related Classifications
HY-119433 Related Classifications
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