Omaveloxolone(RTA-408)

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1474034-05-3

包装与价格：

包装	价格(元)
5mg	电议
25mg	电议

产品介绍

化学性质

Storage	Store at -20°C
M.Wt	554.71
Cas No.	1474034-05-3
Formula	C₃₃H₄₄F₂N₂O₃
Solubility	≥55.5 mg/mL in DMSO; insoluble in H2O; ≥25.05 mg/mL in EtOH
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

Omaveloxolone (RTA-408) is a novel synthetic triterpenoid that binds to Kelch-like ECH-associated protein 1 (Keap1) and attenuate nuclear factor erythroid 2-related factor 2 (Nrf2) degradation [1].

Keap1 is involved in proteasomal degradation of Nrf2, thereby maintaining low basal levels of Nrf2. Binding to Keap1 and blocking its ability to promote Nrf2 degradation increase newly synthesized Nrf2 accumulated in the nucleus where Nrf2 increases the expression of antioxidant genes and decreases the expression of pro-inflammatory genes [1].

In interferon-γ-stimulated RAW 264.7 macrophage cells, low concentrations (≤ 25 nM) of RTA-408 activated Nrf2 and lowered nitric oxide and pro-inflammatory cytokine levels. At higher concentrations, RTA-408 inhibited tumor cell growth, with GI50 of 260 ± 74 nM. Meanwhile, RTA-408 increased caspase activity in tumor cell lines, but not in normal primary human cells.

In mice with radiation-induced dermatitis, topical application of RTA-408 (0.01%, 0.1% and 1.0%, q.d.) resulted in dose-dependent improvements in the appearance of skin, with 1.0% RTA-408 markedly reducing epidermal and collagen thickening, preventing dermal necrosis, and completely alleviating skin ulcers [2].

References:

[1]. Probst B L, Trevino I, McCauley L, et al. RTA 408, a novel synthetic triterpenoid with broad anticancer and anti-inflammatory activity. PLoS One, 2015, 10(4): e0122942.

[2]. Reisman S A, Lee C Y, Meyer C J, et al. Topical application of the synthetic triterpenoid RTA 408 protects mice from radiation-induced dermatitis. Radiation Research, 2014, 181(5): 512-520.

试验操作

细胞实验[1]:
细胞系	PANC-1，A549和A375细胞系
溶解方法	可溶于DMSO。为了获得更高浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。
反应条件	0~1000 nM，72小时
应用	RTA 408可抑制人类肿瘤细胞系的生长，并诱导肿瘤细胞凋亡（增加caspase酶的活性）。
动物实验[2]:
动物模型	BALB/c小鼠
剂量	每天局部涂抹（0.01％，0.1％或1.0％，溶于芝麻油中），持续35天
应用	RTA 408可以通过激活抗氧化转录因子Nrf2和抑制促炎转录因子核因子κB（NF-κB）来保护皮肤免受辐射诱发的皮炎。
注意事项	请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。
References: [1] Probst BL, Trevino I, McCauley L, Bumeister R, Dulubova I, Wigley WC, Ferguson DA. RTA 408, A Novel Synthetic Triterpenoid with Broad Anticancer and Anti-Inflammatory Activity. PLoS One. 2015 Apr 21;10(4):e0122942. [2] Reisman SA, Lee CY, Meyer CJ, Proksch JW, Sonis ST, Ward KW. Topical application of the synthetic triterpenoid RTA 408 protects mice from radiation-induced dermatitis. Radiat Res. 2014 May;181(5):512-20.