Home Immunology & Inflammation Nrf2 activator CDDO-Im (RTA-403)

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CDDO-Im (RTA-403) Nrf2 activator

Cat.No.S9723

An activator of nuclear factor erythroid 2–related factor 2 (Nrf2) and peroxisome proliferator-activated receptor (PPAR), CDDO-Im (RTA-403) binds to PPARα and PPARγ with Ki of 232 nM and 344 nM, respectively. It inhibits inflammatory response and tumor growth in vivo.
CDDO-Im (RTA-403) Nrf2 activator Chemical Structure

Chemical Structure

Molecular Weight: 541.72

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Quality Control

Batch: Purity: 99.23%
99.23

Solubility

In vitro
Batch:

DMSO : 56 mg/mL (103.37 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 541.72 Formula
C34H43N3O3
 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 443104-02-7 -- Storage of Stock Solutions

Synonyms CDDO-Imidazolide, TP-235 Smiles CC1(C)CCC2(CCC3(C)C(C2C1)C(=O)C=C4C5(C)C=C(C#N)C(=O)C(C)(C)C5CCC34C)C(=O)[N]6C=CN=C6

Mechanism of Action

Targets/IC50/Ki
Nrf2
PPARα
(Cell-free assay)
232 nM(Ki)
PPARγ
(Cell-free assay)
344 nM(Ki)
In vitro

CDDO-Im (RTA-403) is highly active in suppressing cellular proliferation of human leukemia and breast cancer cell lines (IC50, 10–30 nM). In U937 leukemia cells, it also induces monocytic differentiation as measured by increased cell surface expression of CD11b and CD36. This compound has significant actions independent of PPAR transactivation.
In vivo

CDDO-Im (RTA-403) is a novel synthetic triterpenoid more potent than its parent compound (CDDO). In vivo, it is a potent inhibitor of de novo inducible nitric oxide synthase expression in primary mouse macrophages. Moreover, this compound inhibits growth of B16 murine melanoma and L1210 murine leukemia cells in vivo.
References

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