S88250 |
CVT-10216 |
源叶(MedMol) | 98% |
- 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: -20℃
- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)