| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
CPUY192018 targets the Keap1-Nrf2 protein-protein interaction. Keap1 is a negative regulator of Nrf2, a transcription factor that controls the expression of antioxidant and cytoprotective genes. By inhibiting the Keap1-Nrf2 interaction, CPUY192018 stabilizes Nrf2, allowing it to translocate to the nucleus and activate the transcription of its target genes, such as NQO1. This leads to enhanced resistance to oxidative stress and cytoprotective effects.
|
|---|---|
| ln Vitro |
In vitro, CPUY192018 is a potent inhibitor of the Keap1-Nrf2 PPI with an IC50 of 0.63 µM. It induces the expression of the Nrf2-dependent gene NQO1 at 100 µM. It shows cytoprotective effects in NCM460 colon cells. It inhibits glycolysis and enhances resistance to oxidative stress.
|
| ln Vivo |
CPUY192018 has been shown to have cytoprotective effects against DSS in mouse colon via the activation of Nrf2 signaling. It can be used to study mitochondrial autophagy. Its ability to activate Nrf2 and enhance resistance to oxidative stress suggests potential therapeutic applications in diseases involving oxidative damage and inflammation.
|
| Enzyme Assay |
CPUY192018 is evaluated in cell-free assays to measure its ability to inhibit the Keap1-Nrf2 interaction. These assays typically involve incubating the compound with purified Keap1 and Nrf2 proteins and measuring the disruption of their binding using techniques such as fluorescence polarization or surface plasmon resonance. IC50 values are determined.
|
| Cell Assay |
CPUY192018 is assessed in cell-based assays using NCM460 colon cells. Cells are treated with CPUY192018, and the expression of Nrf2 target genes, such as NQO1, is measured by qPCR or Western blot analysis. Cytoprotective effects are evaluated by assessing cell viability under oxidative stress conditions. Its effects on glycolysis and mitochondrial autophagy are also studied.
|
| Animal Protocol |
CPUY192018 is administered in animal models to evaluate its cytoprotective effects. It has been shown to have a cytoprotective effect against DSS in mouse colon. Efficacy is assessed by measuring markers of oxidative stress, inflammation, and tissue damage. Its ability to activate Nrf2 signaling in vivo is confirmed by measuring the expression of Nrf2 target genes in tissues.
|
| ADME/Pharmacokinetics |
CPUY192018 has a molecular formula of C28H24N2Na2O10S2 and a molecular weight of 658.6. Its CAS number is 1567836-15-0. The compound is soluble in DMSO at 200 mg/mL. It should be stored under recommended conditions. It is also known as CPUY192018 disodium.
|
| Toxicity/Toxicokinetics |
No detailed toxicity data is available for CPUY192018. The compound is for research use only and is not intended for human therapeutic use. It is a potent Keap1-Nrf2 inhibitor used to study the role of Nrf2 in oxidative stress and cytoprotection.
|
| Additional Infomation |
CPUY192018 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction. It induces the expression of Nrf2-dependent genes and shows cytoprotective effects. It is used in research to study oxidative stress and mitochondrial autophagy. The compound is not approved for clinical use.
|
| Molecular Formula |
C28H26N2O10S2
|
|---|---|
| Molecular Weight |
614.643445491791
|
| Exact Mass |
614.102
|
| CAS # |
1567836-15-0
|
| PubChem CID |
73330369
|
| Appearance |
White to off-white solid powder
|
| LogP |
3.7
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
42
|
| Complexity |
1050
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC1=CC=C(C=C1)S(=O)(=O)N(CC(=O)O)C2=CC=C(C3=CC=CC=C32)N(CC(=O)O)S(=O)(=O)C4=CC=C(C=C4)OC
|
| InChi Key |
KWSIQJUNYMMCTB-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C28H26N2O10S2/c1-39-19-7-11-21(12-8-19)41(35,36)29(17-27(31)32)25-15-16-26(24-6-4-3-5-23(24)25)30(18-28(33)34)42(37,38)22-13-9-20(40-2)10-14-22/h3-16H,17-18H2,1-2H3,(H,31,32)(H,33,34)
|
| Chemical Name |
2-[[4-[carboxymethyl-(4-methoxyphenyl)sulfonylamino]naphthalen-1-yl]-(4-methoxyphenyl)sulfonylamino]acetic acid
|
| Synonyms |
CPUY192018disodium; CPUY192018-disodium; CPUY192018 Disodium
|
| 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 (~406.74 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.38 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.38 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 | 1.6270 mL | 8.1348 mL | 16.2697 mL | |
| 5 mM | 0.3254 mL | 1.6270 mL | 3.2539 mL | |
| 10 mM | 0.1627 mL | 0.8135 mL | 1.6270 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
