同义名 :	-
	CAS号 :	870544-59-5
	货号 :	A286791
	分子式 :	C23H22F3N3O3
	纯度 :	98+%
	分子量 :	445.43
	MDL号 :	MFCD28386231
	存储条件：	Pure form Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	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

[1]Mañé N, Jiménez-Sábado V, Jiménez M. BPTU, an allosteric antagonist of P2Y1 receptor, blocks nerve mediated inhibitory neuromuscular responses in the gastrointestinal tract of rodents. Neuropharmacology. 2016 Nov;110(Pt A):376-385. doi: 10.1016/j.neuropharm.2016.07.033. Epub 2016 Aug 3. PMID: 27496690. [2]Zhang D, Gao ZG, Zhang K, Kiselev E, Crane S, Wang J, Paoletta S, Yi C, Ma L, Zhang W, Han GW, Liu H, Cherezov V, Katritch V, Jiang H, Stevens RC, Jacobson KA, Zhao Q, Wu B. Two disparate ligand-binding sites in the human P2Y1 receptor. Nature. 2015 Apr 16;520(7547):317-21. doi: 10.1038/nature14287. Epub 2015 Mar 30. PMID: 25822790; PMCID: PMC4408927. [3]Yuan X, Raniolo S, Limongelli V, Xu Y. The Molecular Mechanism Underlying Ligand Binding to the Membrane-Embedded Site of a G-Protein-Coupled Receptor. J Chem Theory Comput. 2018 May 8;14(5):2761-2770. doi: 10.1021/acs.jctc.8b00046. Epub 2018 Apr 27. PMID: 29660291.