产品说明书
BpV(HOpic)
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同义名 : | Bisperoxovanadium(HOpic);HOpic;bpV(HOpic) (potassium salt);bpV |
| CAS号 : | 722494-26-0 | |
| 货号 : | A189911 | |
| 分子式 : | C6H4K2NO8V | |
| 纯度 : | 95% | |
| 分子量 : | 347.236 | |
| MDL号 : | MFCD01862576 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 2 mg/mL(5.76 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 50 mg/mL(143.99 mM)，配合低频超声，并水浴加热至45℃助溶 |
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| 动物实验配方： |
PO 0.5% CMC-Na 46 mg/mL clear |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The phosphatase and tensin homologue deleted on chromosome 10 (PTEN) is a tumor suppressor that inhibit cell survival and proliferation by inactivating PI 3-kinase-dependent signaling pathway. bpV (HOpic) is a vanadate derivative that inhibits PTEN with an IC50 value of 14 nM. In primary cardiomyocytes incubated with bpV (HOpic) without the exposure to simulated ischemia-reperfusion (SIR) for 2 hours, bpV (HOpic) at 10, 15, and 20 μM decreased the percentage of trypan-positive cells compared with non-bpV-treated cells. The maximal effect of bpV (HOpic) on the suppression of cell death was achieved at 15 μM. The cell viability as measured by MTT assay was significantly improved by bpV (HOpic) at 5 – 20 μM in cells with or without SIR. The effect of bpV (HOpic) on cardiomyocytes apoptosis was determined by TUNEL assay, in which bpV (HOpic) at 10, 15, and 20 μM decreased apoptosis in cells without SIR, whereas the anti-apoptotic effect of bpV (HOpic) in cells exposed to SIR was observed at 5, 10, and 15 μM. In rats received bpV (HOpic) before I30m and R4h, the myocardial infarct size was reduced compared to control group, and the maximal effect of bpV (HOpic) was achieved at 1.0 mg/kg. However, the protective effect of bpV (HOpic) on reducing myocardial infarct size was abrogated by wortmannin and L-NAME. In rats treated with bpV (HOpic) (1.0 mg/kg) either before ischemia (BpV-BI) or before reperfusion (BpV-BR), bpV (HOpic) reduced the increase of the left ventricular internal diameter in diastole and in systole after the I/R injury. In rats received 1.0 mg/kg bpV (HOpic) one hour before ischemia, the PTEN activity was significantly reduced at 30 m of ischemia and 4 and 12h of reperfusion. | ||
| 作用机制 | bpV (HOpic) acts a PTEN inhibitor by interacting with the active center of PTEN, the CX5R motif. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02496598 | Primary Ovarian Insufficiency ... 展开 >> Infertility 收起 << | Not Applicable | Terminated(Results were not pr... 展开 >>omising) 收起 << | - | United States, Colorado ... 展开 >> Fertility Laboratories of Colorado Lone Tree, Colorado, United States, 80124 National Foundation for Fertility Research Lone Tree, Colorado, United States, 80124 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.88mL 0.58mL 0.29mL |
14.40mL 2.88mL 1.44mL |
28.80mL 5.76mL 2.88mL |
