Omaveloxolone (RTA 408) is a first-in-class antioxidant inflammatory modulator (AIM) that activates Nrf2 and inhibits nitric oxide (NO). Omaveloxolone inhibits osteoclastogenesis by inhibiting the STING-dependent NF-κb signaling pathway.
Omaveloxolone (RTA-408) is a member of the synthetic oleanane triterpenoid class of compounds and an activator of nuclear factor erythroid 2 [NF-E2]-related factor 2 (Nrf2). Omaveloxolone (RTA-408) potently increases expression of Nrf2 target genes and reverses IFNγ-mediated suppression of Gclc expression in RAW 264.7 cells. In a panel of eight human tumor cell lines, Omaveloxolone inhibits growth with an average GI50 value of 260 nM and induces apoptosis.
J Cancer Res Clin Oncol. 2023 Apr 29.
Apatinib combined with olaparib induces ferroptosis via a p53-dependent manner in ovarian cancer
Omaveloxolone purchased from AbMole
| Molecular Weight | 554.71 |
| Formula | C33H44F2N2O3 |
| CAS Number | 1474034-05-3 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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