| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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CDDO-Im (CDDO-imidazolide; TP235; RTA403) is a novel and potent activator of Nrf2 and PPAR signaling with Kis of 232 and 344 nM for PPARα and PPARγ. It is able to increase Nrf2 protein expression and enhances Nrf2-dependent cytoprotective gene expression. It inhibits cell growth and induces apoptosis of pancreatic cancer cells in vitro and also reduces acetaminophen-induced liver injury in mice.
| ln Vitro |
In human leukemia and breast cancer cell lines, CDDO-Im is highly active (IC50 = 10–30 nM) at suppressing cell proliferation. Moreover, CDDO-Im promotes monocyte development in U937 leukemia cells, as evidenced by elevated expression of CD11b and CD36 on the cell surface [1]. Treatment with CDDO-Im raises Nrf2 protein levels, a transcription factor that has been proven to bind ARE sequences in the past, and promotes the expression of numerous Nrf2-regulated genes related to detoxification and antioxidants [2]. One of the most effective synthetic triterpenoids, CDDO-Im causes apoptosis and growth suppression in a range of human cancer cells, including breast, lung, pancreatic, and multiple myeloma. Three-negative breast cancer cell lines, SUM159 and MDA-MB-231, showed significant increases in cell cycle arrest in the G2/M phase and apoptosis upon treatment with CDDO-Im. In SUM159 tumorspheres, CDDO-Im therapy dramatically reduced CD24-/EpCAM+ cells. In primary and secondary spheroid cultures, CDDO-Im also markedly decreased tumorsphere size and spheroid formation efficiency [3].
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| ln Vivo |
In primary murine macrophages, CDDO-Im is a strong inhibitor of de novo inducible nitric oxide synthase production. Moreover, CDDO-Im impeded the in vivo development of L1210 murine leukemia cells and B16 murine melanoma cells. The capacity of IFN-γ to produce iNOS was almost totally prevented by injection of 10 nM (5.4 μg) CDDO-Im, whereas treatment with only 1 nmol CDDO-Im (0.54 μg) was only partially successful [1].
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| References |
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| Molecular Formula |
C₃₄H₄₃N₃O₃
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|---|---|
| Molecular Weight |
541.74
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| Exact Mass |
541.33
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| CAS # |
443104-02-7
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| PubChem CID |
9958995
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| Appearance |
White to off-white solid powder
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| LogP |
6.742
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
40
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| Complexity |
1310
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| Defined Atom Stereocenter Count |
7
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| SMILES |
C[C@@]12CC[C@]3(CCC(C[C@H]3[C@H]1C(=O)C=C4[C@]2(CC[C@@H]5[C@@]4(C=C(C(=O)C5(C)C)C#N)C)C)(C)C)C(=O)N6C=CN=C6
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| InChi Key |
ITFBYYCNYVFPKD-FMIDTUQUSA-N
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| InChi Code |
InChI=1S/C34H43N3O3/c1-29(2)10-12-34(28(40)37-15-14-36-20-37)13-11-33(7)26(22(34)18-29)23(38)16-25-31(5)17-21(19-35)27(39)30(3,4)24(31)8-9-32(25,33)6/h14-17,20,22,24,26H,8-13,18H2,1-7H3/t22-,24-,26-,31-,32+,33+,34-/m0/s1
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| Chemical Name |
1-(2-Cyano-3,12,28-trioxooleana-1,9(11)-dien-28-yl)-1H-imidazole
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| Synonyms |
RTA-403; TP-235; RTA403; TP235; RTA 403; TP 235; CDDO Im, CDDO Imidazolide
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~46.15 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (4.61 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: 2.5 mg/mL (4.61 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 25.0 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: ≥ 2.5 mg/mL (4.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2.5 mg/mL (4.61 mM) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: 2.5 mg/mL (4.61 mM) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8459 mL | 9.2295 mL | 18.4590 mL | |
| 5 mM | 0.3692 mL | 1.8459 mL | 3.6918 mL | |
| 10 mM | 0.1846 mL | 0.9230 mL | 1.8459 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.
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