CDDO-EA (Synonyms: CDDO ethyl amide; TP319; RTA 405) |
| Katalog-Nr.GC35630 |
CDDO-EA ist ein mit NF-E2 verwandter Faktor 2/antioxidatives Response-Element (Nrf2/ARE)-Aktivator.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 932730-51-3
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
CDDO-EA is an NF-E2 related factor 2/antioxidant response element (Nrf2/ARE) activator. Nrf2/ARE[1]
CDDO-EA potently activates Nrf2/ARE in a cell culture model of ALS and in the G93A SOD1 mouse model of ALS[1]. CDDO-EA is a potent inducer of apoptosis in A549 lung cancer cells, as shown both by PARP cleavage and Annexin staining. CDDO-EA is more potent than CDDO itself as inducers of heme oxygenase-1 (HO-1). In RAW264.7 macrophage-like cells, CDDO-EA is 7-fold more potent than CDDO as suppressors of the ability of IFN-γ to induce iNOS[2].
The survival analysis shows that G93A mice treated with CDDO-EA, compared to G93A littermate controls, lives significantly longer. CDDO-EA treatment increases the life-span by 20.6 days from 124.05±3.7 days to 144.72±8.1 days (16.6%) (p<0.001). In CDDO-EA-treated G93A mice, the age of death is 141.4±5.2 days and the duration from the age of onset to the age of death is 57.6±7.6 days, which means that the age of death from onset is prolonged by 17.5 days (43%)[1].
[1]. Neymotin A, et al. Neuroprotective effect of Nrf2/ARE activators, CDDO ethylamide and CDDO trifluoroethylamide, in a mouse model of amyotrophic lateral sclerosis. Free Radic Biol Med. 2011 Jul 1;51(1):88-96. [2]. Liby K, et al. The synthetic triterpenoids CDDO-methyl ester and CDDO-ethyl amide prevent lung cancer induced by vinyl carbamate in A/J mice. Cancer Res. 2007 Mar 15;67(6):2414-9.
Cell experiment: | Wild-type and Nrf2−/− mouse embryonic fibroblasts are pre-treated with CDDO-EA or CDDO-TFEA at various concentrations (1, 10 and 100 nM in DMSO) for 18 hours and incubated with 2’,7’-Dichlorodihydrofluorecein diacetate (H2DCFDA) for 30 min. Cells are challenged with 250 µM tBHP for 15-30 min and the mean fluorescence intensity for ~10,000 cells is analyzed by FACSan flow cytometry using a 480-nm excitation wavelength and a 525-nm emission wavelength[1]. |
Animal experiment: | Mice[1] G93A SOD1 transgenic familial ALS mice (high copy number) B6SJL background strain (G93A SOD1, B6SJL-TgGur1) are used. G93A transgenic mice are assigned randomly to the control (vehicle, mouse chaw only) and to mouse chaw containing either CDDO-EA or CDDO-TFEA (400 mg/kg of food, n=30 in both groups). This dose corresponds to about 80 mg/kg body weight/day, assuming each mouse consumes 5 grams of food per day. We found mice can tolerate this dose. Treatments started at two different time regimens: 1) “Early” at 30 days of age, about two months prior to symptom onset; 2) “At Onset” from the onset of the phenotype (80-90 days of age). A diet consisting of either 400 mg of CDDO-TFEA per kg of food or 400 mg of CDDO-EA per kg of food, and a control lab diet, are prepared by Purina. |
References: [1]. Neymotin A, et al. Neuroprotective effect of Nrf2/ARE activators, CDDO ethylamide and CDDO trifluoroethylamide, in a mouse model of amyotrophic lateral sclerosis. Free Radic Biol Med. 2011 Jul 1;51(1):88-96. | |
| Cas No. | 932730-51-3 | SDF | |
| Überlieferungen | CDDO ethyl amide; TP319; RTA 405 | ||
| Canonical SMILES | O=C1C(C#N)=C[C@@]2(C)[C@](CC[C@]([C@@]3(C)[C@@]4([H])[C@@]5([H])[C@@](CCC(C)(C)C5)(C(NCC)=O)CC3)(C)C2=CC4=O)([H])C1(C)C | ||
| Formula | C33H46N2O3 | M.Wt | 518.73 |
| Löslichkeit | DMSO: ≥ 34 mg/mL (65.54 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9278 mL | 9.6389 mL | 19.2779 mL |
| 5 mM | 0.3856 mL | 1.9278 mL | 3.8556 mL |
| 10 mM | 0.1928 mL | 0.9639 mL | 1.9278 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 7 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *