CDDO-Im (RTA-403)
(Synonyms: RTA-403; TP-235; CDDO-Imidazolide) 目录号 : GC32723
An activator of Nrf2 signaling
Cas No.:443104-02-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
CDDO-Im is a synthetic triterpenoid and an activator of Nrf2 signaling.1,2 It binds to Keap1, inhibiting the degradation of Nrf2 and leading to increased Nrf2 protein levels.2 CDDO-Im (100 nM) increases the expression of Nrf2 target genes and activates heme oxygenase-1 (HO-1) in a reporter assay using CV-1 cells.1 It also binds to PPARγ and PPARα (Kis = 344 and 232 nM, respectively) and induces PPARγ transactivation in SW480 cells.3,4 It inhibits the production of nitric oxide synthase (NOS) in isolated mouse macrophages (IC50 = 0.014 nM).5 CDDO-Im (300 nM) inhibits proliferation of U937 and MCF-7 cells and reduces fatty acid synthesis in LiSa-2 human liposarcoma cells when used at a concentration of 100 nM.3,6 It reduces tumor growth in a B16 murine melanoma model when administered at a dose of 50 ?g/animal twice per day.3
1.Liby, K., Hock, T., Yore, M.M., et al.The synthetic triterpenoids, CDDO and CDDO-imidazolide, are potent inducers of heme oxygenase-1 and Nrf2/ARE signalingCancer Res.65(11)4789-4798(2005) 2.Meng, X., Waddington, J.C., Tailor, A., et al.CDDO-imidazolide targets multiple amino acid residues on the Nrf2 adaptor, Keap1J. Med. Chem.63(17)9965-9976(2020) 3.Place, A.E., Suh, N., Williams, C.R., et al.The novel synthetic triterpenoid, CDDO-imidazolide, inhibits inflammatory response and tumor growth in vivoClin. Cancer Res.9(7)2798-2806(2003) 4.Chintharlapalli, S., Papineni, S., Konopleva, M., et al.2-Cyano-3,12-dioxoolean-1,9-dien-28-oic acid and related compounds inhibit growth of colon cancer cells through peroxisome proliferator-activated receptor γ-dependent and -independent pathwaysMol. Pharmacol.68(1)119-128(2005) 5.Honda, T., Honda, Y., Favaloro, F.G., Jr., et al.A novel dicyanotriterpenoid, 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-onitrile, active at picomolar concentrations for inhibition of nitric oxide productionBioorg. Med. Chem. Lett.12(7)1027-1030(2002) 6.Hughes, D.T., Martel, P.M., Knlaw, W.B., et al.The synthetic triterpenoid CDDO-Im inhibits fatty acid synthase expression and has antiproliferative and proapoptotic effects in human liposarcoma cellsCancer Invest.26(2)118-127(2009)
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.846 mL | 9.2299 mL | 18.4597 mL |
| 5 mM | 0.3692 mL | 1.846 mL | 3.6919 mL |
| 10 mM | 0.1846 mL | 0.923 mL | 1.846 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。