| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg | |||
| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
Apoptosis and necroptosis pathways. CDDO-3P-Im is an orally active inhibitor of necroptosis with chemopreventive effects. It modulates cell death pathways, potentially through the regulation of quinone reductase (NQO1) and heme oxygenase-1 (HO-1).
|
|---|---|
| ln Vitro |
U937 cells are induced to differentiate at 30 nM by CDDO-3P-Im (30-100 nM; 4 days) [1]. With an IC50 of 4.3 nM, CDDO-3P-Im suppresses the generation of NO in RAW264.7 cells[1].
CDDO-3P-Im (30 nM) induces differentiation of U937 cells. In various animal tissues, the compound dramatically elevates the levels of quinone reductase (NQO1) and heme oxygenase-1 (HO-1) mRNA and protein. These effects contribute to its chemopreventive and cytoprotective activities. |
| ln Vivo |
CDDO-3P-Im was found to be more stable than CDDO-Im in pharmacokinetic investigations [1]. In a variety of animal tissues in vivo, CDDO-3P-Im dramatically raises the levels of quinone reductase (NQO1) and heme oxygenase-1 (HO-1) mRNA and protein [1]. In A/J mice, CDDO-3P-Im (50–200 mg/kg; diet; 16 weeks) decreases the quantity, size, and severity of tumors [1].
CDDO-3P-Im reduces the size and severity of lung tumors in a mouse lung cancer model. In A/J mice, the compound demonstrates chemopreventive effects, decreasing tumor burden. These in vivo findings support its potential as a cancer chemopreventive agent. |
| Enzyme Assay |
Cell-based assays are performed using U937 cells to evaluate differentiation. Cells are treated with CDDO-3P-Im at 30 nM, and differentiation markers are assessed. In RAW264.7 cells, the compound's effects on inflammatory responses and cell death pathways are evaluated.
|
| Cell Assay |
Apoptosis analysis [1]
Cell Types: U937 Cell Tested Concentrations: 30 nM, 100 nM Incubation Duration: 4 days Experimental Results: 30 nM induced U937 cell differentiation. In vitro cell assays include the evaluation of CDDO-3P-Im in U937 cells at 30 nM to assess differentiation. In RAW264.7 cells, the compound's activity is assessed to understand its mechanism of action on inflammatory and cell death pathways. |
| Animal Protocol |
Animal/Disease Models: Sevenweeks old female A/J mice [1]
Doses: 50 mg/kg, 200 mg/kg Route of Administration: diet; continued for 16 weeks Experimental Results: The number, size and severity of tumors were diminished. In vivo studies are performed in A/J mouse models of lung cancer. CDDO-3P-Im is administered orally at doses of 50–200 mg/kg, and tumor size, severity, and biomarkers such as NQO1 and HO-1 are assessed. The compound's chemopreventive efficacy is evaluated by measuring tumor burden. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of CDDO-3P-Im have been characterized in preclinical studies. The compound is orally active, as demonstrated by its efficacy following oral administration in mouse models. Detailed PK parameters would require further investigation from primary literature.
|
| Toxicity/Toxicokinetics |
Comprehensive toxicity data for CDDO-3P-Im are not extensively detailed in the available literature. The compound is intended for research use only. Its chemopreventive and cytoprotective effects suggest a favorable safety profile, but further toxicological studies would be needed.
|
| References |
[1]. Cao M , et al. Novel synthetic pyridyl analogues of CDDO-Imidazolide are useful new tools in cancer prevention. Pharmacol Res. 2015 Oct;100:135-47.
[2]. Yuanyuan Wang, et al. Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors. Eur J Med Chem. 2020 Nov 21;113030. |
| Additional Infomation |
CDDO-3P-Im is a research compound used in cancer prevention and necroptosis studies. It is a synthetic triterpenoid analogue with potential therapeutic applications in ischemia/reperfusion injury. The compound is not approved for clinical use and is supplied for research purposes only.
|
| Molecular Formula |
C39H46N4O3
|
|---|---|
| Molecular Weight |
618.807549953461
|
| Exact Mass |
618.356
|
| CAS # |
1883650-95-0
|
| PubChem CID |
135397766
|
| Appearance |
White to off-white solid powder
|
| LogP |
7.1
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
46
|
| Complexity |
1480
|
| Defined Atom Stereocenter Count |
7
|
| 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=C(N=C6)C7=CN=CC=C7
|
| InChi Key |
GXKRPLQWYWDFQN-CXUPGZSSSA-N
|
| InChi Code |
InChI=1S/C39H46N4O3/c1-34(2)12-14-39(33(46)43-22-27(42-23-43)24-9-8-16-41-21-24)15-13-38(7)31(26(39)19-34)28(44)17-30-36(5)18-25(20-40)32(45)35(3,4)29(36)10-11-37(30,38)6/h8-9,16-18,21-23,26,29,31H,10-15,19H2,1-7H3/t26-,29-,31-,36-,37+,38+,39-/m0/s1
|
| Chemical Name |
(4aR,6aR,6aS,6bR,8aS,12aS,14bS)-4,4,6a,6b,11,11,14b-heptamethyl-3,13-dioxo-8a-(4-pyridin-3-ylimidazole-1-carbonyl)-4a,5,6,6a,7,8,9,10,12,12a-decahydropicene-2-carbonitrile
|
| Synonyms |
CDDO3PIm; CDDO 3P Im
|
| 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 : ~250 mg/mL (~404.00 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.36 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6160 mL | 8.0800 mL | 16.1600 mL | |
| 5 mM | 0.3232 mL | 1.6160 mL | 3.2320 mL | |
| 10 mM | 0.1616 mL | 0.8080 mL | 1.6160 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
