| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Prinaberel, formerly known as ERB-041, is a biochemical which acts as a highly selective agonist of the ERβ subtype of the estrogen receptor. It is used in scientific research to elucidate the role of the ERβ receptor. Studies have indicated that selective ERβ agonists like prinaberel could be useful in the clinical treatment of a variety of medical conditions including inflammatory bowel disease, rheumatoid arthritis, endometriosis, and sepsis. Accordingly, prinaberel either was or still is under investigation by Wyeth for the treatment of some of these conditions.
| ln Vitro |
Prinaberel (ERB-041) (0-60 µM; 24 hours) treatment of human SCC cells results in reduced colony formation, cell differentiation, and cell cycle arrest [2]. In A431 cells, prinaberel significantly decreased the expression of inflammatory regulatory proteins as p-NFκBp65, iNOS, and COX-2. Phosphorylated PI3K and AKT are decreased by prinaberel, which is linked to increased E-cadherin expression and decreased A431 cell motility [2]. Cell growth is inhibited by prinaberel (0.01-10 µM) in a dose- and time-dependent manner [3]. Prinaberel (10 µM; 48 hours) induces ovarian cancer (SKOV-3 cells) to undergo apoptosis [3].
|
|---|---|
| ln Vivo |
In SKH-1 hairless mice, the topical drug prinaberel (2 mg/mouse; 30 minutes prior to UVB irradiation for 30 weeks) prevents the growth of squamous cell carcinoma [2]. Prinaberel causes apoptosis and inhibits UVB-induced proliferation and angiogenesis in skin cancers. In skin cancers caused by UVB radiation, prinaberel suppresses pro-inflammatory signaling pathways. Plinabiber inhibits WNT signaling and the PI3K-AKT pathway to reduce tumor invasiveness [2].
|
| Cell Assay |
Western Blot Analysis[2]
Cell Types: A431 Cell Tested Concentrations: 0, 20, 40 and 60 µM Incubation Duration: 24 hrs (hours) Experimental Results: diminished expression of G1 cyclins (D1, D2 and D3) and CDK4. Cell proliferation assay[3] Cell Types: SKOV-3, A2780CP or OVCAR-3 Cell Tested Concentrations: 0.01, 0.1 and 10 µM Incubation Duration: 24-48 hrs (hours) Experimental Results: Significant inhibitory effect on cell proliferation. |
| Animal Protocol |
Animal/Disease Models: Six to eight week old SKH-1 hairless female mice [2]
Doses: 2 mg/mouse in 200 µl ethanol UVB (180mJ/cm2) 30 minutes before irradiation for 30 weeks Experimental Results: SKH -1 diminished UVB-induced skin tumor development in hairless mice. |
| References |
|
| Additional Infomation |
Prinaberel is an estrogen receptor beta agonist.
|
| Molecular Formula |
C15H10FNO3
|
|---|---|
| Molecular Weight |
271.24
|
| Exact Mass |
271.064
|
| CAS # |
524684-52-4
|
| Related CAS # |
524684-52-4;
|
| PubChem CID |
656954
|
| Appearance |
White to gray solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
451.6±45.0 °C at 760 mmHg
|
| Melting Point |
250-252ºC
|
| Flash Point |
226.9±28.7 °C
|
| Vapour Pressure |
0.0±1.1 mmHg at 25°C
|
| Index of Refraction |
1.695
|
| LogP |
3.97
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
20
|
| Complexity |
367
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
MQIMZDXIAHJKQP-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C15H10FNO3/c1-2-8-5-10(18)7-12-14(8)20-15(17-12)9-3-4-13(19)11(16)6-9/h2-7,18-19H,1H2
|
| Chemical Name |
2-(3-fluoro-4-hydroxyphenyl)-7-vinylbenzo[d]oxazol-5-ol
|
| Synonyms |
ERB041 ERB 041 ERB041 Prinaberel WAY-202041 WAY202041 WAY 202041
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ≥ 40 mg/mL (~147.47 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (18.43 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 50.0 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: 5 mg/mL (18.43 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 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: ≥ 5 mg/mL (18.43 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 | 3.6868 mL | 18.4339 mL | 36.8677 mL | |
| 5 mM | 0.7374 mL | 3.6868 mL | 7.3735 mL | |
| 10 mM | 0.3687 mL | 1.8434 mL | 3.6868 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 |
| NCT00316459 | COMPLETED | Drug: ERB-041 | Healthy Long QT Syndrome |
Wyeth is now a wholly owned subsidiary of Pfizer | 2006-05 | Phase 1 |
| NCT00275379 | WITHDRAWN | Drug: ERB-041 | Cystitis, Interstitial | Wyeth is now a wholly owned subsidiary of Pfizer | 2006-08 | Not Applicable |
| NCT00434187 | COMPLETED | Drug: ERB-041 | Healthy | Wyeth is now a wholly owned subsidiary of Pfizer | 2006-08 | Phase 1 |
| NCT00245947 | COMPLETED | Drug: ERB-041 | Crohn's Disease | Wyeth is now a wholly owned subsidiary of Pfizer | 2004-04 | Phase 1 |
| NCT00141830 | COMPLETED | Drug: Methotrexate plus ERB-041 for 12 weeks Drug: Placebo for 12 weeks |
Rheumatoid Arthritis | Wyeth is now a wholly owned subsidiary of Pfizer | 2005-08 | Phase 2 |
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
