(Rac)-Acolbifene (Synonyms: EM-343; (Rac)-EM-652) |
| رقم الكتالوجGC61488 |
(Rac) -Acolbifene (EM-343 ؛ (Rac) -EM-652) هو الشكل العنصري لـ EM652 (مضادات مستقبلات هرمون الاستروجين) ، له أنشطة مضادة للاستروجين والاستروجين(Rac) -Acolbifene (EM-343 ؛ (Rac) -EM-652) يحتوي على حلقة بيبيريدين ، ويظهر ملفًا شخصيًا دوائيًا جيدًا ، وتقارب ارتباط نسبي (RBA) = 380
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 151533-34-5
Sample solution is provided at 25 µL, 10mM.
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(Rac)-Acolbifene (EM-343; (Rac)-EM-652) is the racemic form of EM652 (estrogen receptor antagonist), has anti-estrogenic and estrogenic activities. (Rac)-Acolbifene (EM-343; (Rac)-EM-652) contains a piperidine ring, shows good pharmacological profile,relative binding affinity (RBA)=380[1].
(Rac)-Acolbifene (EM-343; (Rac)-EM-652) shows a inhibitory effect in T-47D cells with an IC50 value of 0.110 nM[1]. Cell Viability Assay[1] Cell Line: T-47D cells
(Rac)-Acolbifene (orally adminstration; 7.5 nM, 75 nM; 9 days; once daily) shows a good pharmacological profile in ovariectomized mice, shows 63% and 84% antiuterotrophic inhibitions at the 7.5 and 75 nM doses, respectively (PK study, ovariectomized mice)[1].
[1]. Gauthier S1,et al.Synthesis and structure-activity relationships of analogs of EM-652 (acolbifene), a pure selective estrogen receptor modulator. Study of nitrogen substitution.J Enzyme Inhib Med Chem. 2005 Apr;20(2):165-77.
| Cas No. | 151533-34-5 | SDF | |
| المرادفات | EM-343; (Rac)-EM-652 | ||
| Canonical SMILES | OC1=CC=C2C(C)=C(C3=CC=C(O)C=C3)C(C4=CC=C(OCCN5CCCCC5)C=C4)OC2=C1 | ||
| Formula | C29H31NO4 | M.Wt | 457.56 |
| الذوبان | DMSO: 100 mg/mL (218.55 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1855 mL | 10.9275 mL | 21.8551 mL |
| 5 mM | 437.1 μL | 2.1855 mL | 4.371 mL |
| 10 mM | 218.6 μL | 1.0928 mL | 2.1855 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)
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