产品说明书
BPTU
 |
同义名 : | - |
| CAS号 : | 870544-59-5 | |
| 货号 : | A286791 | |
| 分子式 : | C23H22F3N3O3 | |
| 纯度 : | 98+% | |
| 分子量 : | 445.434 | |
| MDL号 : | MFCD28386231 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 35 mg/mL(78.57 mM)，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 |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | BPTU is a P2Y1 allosteric antagonist as an antithrombotic agent, which binds receptor entirely outside of the helical bundle. BPTU dose-dependently inhibited purinergic inhibitory junction potentials and inhibition of spontaneous motility induced by electrical field stimulation in the colon of rats (EC50 = 0.3 μM) and mice (EC50 = 0.06 μM) [1].BPTU blocked colon nicotine induced relaxation in the rat colon[1]. In the rat colon, the P2Y agonist ADPβS at 10 μM significantly reduces spontaneous contractions, and this reduction is blocked by BPTU at a concentration of 3 μM[1]. Also, the selective P2Y1 agonist MRS2365, at a concentration of 5 μM significantly reduces spontaneous contractions in the murine colon, and this reduction is blocked by BPTU at a concentration of 3 μM[1].BPTU binds to an allosteric pocket on the external receptor interface with the lipid bilayer, located entirely outside of the helical bundle[2]. BPTU prefers partitioning into the interface of polar/lipophilic region of the lipid bilayer before associating with the receptor[3]. Then, it interacts with the second extracellular loop of the receptor and reaches the binding site through the lipid-receptor interface[3]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.25mL 0.45mL 0.22mL |
11.23mL 2.25mL 1.12mL |
22.45mL 4.49mL 2.25mL |
| 参考文献 |
|---|