ERA63 |
| رقم الكتالوجGC31788 |
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 343248-86-2
Sample solution is provided at 25 µL, 10mM.
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ERA63 is a selective estrogen receptor α agonist.
The pharmacologic properties for the ERα agonist ERA-63 (Org 37663) have been shown efficacy in inflammatory models at 1.5 mg/kg. ERA-63 dose-dependently decreases the TT-specific response whereas treatment with the ERβ-agonist ERB-79 has no effect on TT-specific swelling. ERA-63 inhibits the tetanus toxoid (TT)-specific DTH response in WT and ERβ-/- mice but not in ERα-/- mice. ERA-63 inhibits the tetanus-specific delayed type hypersensitivity response in WT and ERβKO but not in the ERαKO mice. Therapeutic administration of the selective agonist ERA-63 decreases the clinical signs of arthritis dose-dependently. In addition, the AUC analysis over the 20-day treatment period reveals a significant dose-dependent reduction in the ERA-63-treated mice when compared with vehicle control[1]. After 28 days of treatment with dosages ranging from pharmacological up to clearly toxic levels, selected ERA-63 dose levels (0.167-0.2, 1.67-2 and 16.7-20 mg/kg) are expected to have comparable estrogenic activity to respective EE dose levels (0.05, 0.5 and 5 mg/kg)[2].
[1]. Dulos J, et al. Suppression of the inflammatory response in experimental arthritis is mediated via estrogen receptor alpha but not estrogen receptor beta. Arthritis Res Ther. 2010;12(3):R101. [2]. Janssen GB, et al. The evaluation of the immunomodulating properties of ERA-63 a pharmaceutical with estrogenic activity. Toxicol Lett. 2008 Aug 28;180(3):196-201.
| Cas No. | 343248-86-2 | SDF | |
| Canonical SMILES | C#C[C@]1(O)CC[C@@]2([H])[C@]3([H])[C@H](C)CC4=C(CCC(C4)=C)[C@@]3([H])CC[C@]12C | ||
| Formula | C22H30O | M.Wt | 310.47 |
| الذوبان | Soluble in DMSO | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.2209 mL | 16.1046 mL | 32.2092 mL |
| 5 mM | 644.2 μL | 3.2209 mL | 6.4418 mL |
| 10 mM | 322.1 μL | 1.6105 mL | 3.2209 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)
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