| 产品描述: | CVT-10216是一种高选择性、可逆的ALDH-2抑制剂,IC50为29 nM |
| 靶点: |
ALDH-2:29 nM; ALDH-1:1.3 μM |
| 体外研究: |
CVT-10216 significantly reduces about 50% of aldehyde dehydrogenase (ALDH) activity in OCI-AML3 cells even in the presence of recombinant TGF-β1 or BM-MSCs, sensitizing cells to chemotherapy. |
| 体内研究: |
CVT-10216, a highly selective, reversible inhibitor of ALDH-2, exhibits both acute and prophylactic inhibitions of repeated alcohol-withdrawal-induced anxiety, which counteracts anxiogenic behavior induced by the benzodiazepine receptor inverse agonist in dose-dependently way |
| 细胞实验: |
Cell lines: OCI-AML3 cells Concentrations: 250, 500 nM, 1, 2 µM Incubation Time: 3 days Method: OCI-AML3 cells are co-cultured with MSCs (200000 cells/well density) and treated with CVT-10216 for 3 days in the presence or absence of recombinant TGF-β1 (5 ng/mL). ALDH activity is measured by ALDEFLUOR assay using flow cytometry. |
| 动物实验: |
Animal Models: FH, iP and Sprague Dawley (SD) rats Dosages: 3.75, 7.5, or 15 mg/kg Administration: i.p. |
| 参考文献: |
1. Arolfo MP, et al. Suppression of heavy drinking and alcohol seeking by a selective ALDH-2 inhibitor. Alcohol Clin Exp Res. 2009 Nov;33(11):1935-44. 2. Yuan B, et al. Bone marrow stromal cells induce an ALDH+ stem cell-like phenotype and enhance therapy resistance in AML through a TGF-β-p38-ALDH2 pathway. PLoS One. 2020 Nov 30;15(11):e0242809. 3. Overstreet DH, et al. A selective ALDH-2 inhibitor reduces anxiety in rats. Pharmacol Biochem Behav. 2009 Dec;94(2):255-61. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.148 ml |
10.742 ml |
21.483 ml |
| 5 mM |
0.43 ml |
2.148 ml |
4.297 ml |
| 10 mM |
0.215 ml |
1.074 ml |
2.148 ml |
| 50 mM |
0.043 ml |
0.215 ml |
0.43 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |