CAS:870544-59-5BPTU

BPTU allosteric antagonist of P2Y1 wtih IC50 of 0.06-0.3 μM with antithrombotic effect and reduces platelet aggregation.

规格	价格	促销价格	库存

18817579266

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咨询

18817579266

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实验数据

技术信息

CAS号

870544-59-5

储存条件

分子式

C23H22F3N3O3

运输

蓝冰

分子量

445.43

别名

溶解度

DMSO	30.0 mg/mL (67.3 mM)
Water	Insoluble

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).BPTU blocked colon nicotine induced relaxation in the rat colon. 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. 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.BPTU binds to an allosteric pocket on the external receptor interface with the lipid bilayer, located entirely outside of the helical bundle. BPTU prefers partitioning into the interface of polar/lipophilic region of the lipid bilayer before associating with the receptor. Then, it interacts with the second extracellular loop of the receptor and reaches the binding site through the lipid-receptor interface.