同义名 :	-
	CAS号 :	790663-33-1
	货号 :	A1166381
	分子式 :	C15H20N4O2S
	纯度 :	99%+
	分子量 :	320.41
	MDL号 :	MFCD32666996
	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	Glutaminyl cyclase (QC) catalyzes the intramolecular cyclization of N-terminal glutamine residues to pyroglutamic acid (pGlu) under liberation of ammonia. Some peptide hormones, such as tyrotropin releasing hormone (TRH) and gonadotropin releasing hormone (GnRH), require the pGlu on the N-terminus for their biological activity. PBD-150, a potent human QC (hQC) inhibitor, shows a remarkable inhibitory power, exhibiting a Ki value of 60 nM[1]. Moreover, PBD150 was able to reduce the deposition of pyroglutamate-modified amyloid-β peptides in brain of transgenic mouse models of Alzheimer disease, leading to a significant improvement of learning and memory in those transgenic animals[2].
作用机制	The essential H-bond donor function is found in PBD-150, pointing toward an interaction with a hydrophobic pocket. And the donor nitrogen of PBD-150 matches the C-terminal amide nitrogen of glutamine[1].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	3.12mL 0.62mL 0.31mL	15.61mL 3.12mL 1.56mL	31.21mL 6.24mL 3.12mL

参考文献

[1]Buchholz M, Heiser U, Schilling S, Niestroj AJ, Zunkel K, Demuth HU. The first potent inhibitors for human glutaminyl cyclase: synthesis and structure-activity relationship. J Med Chem. 2006;49(2):664-677 [2]Huang KF, Liaw SS, Huang WL, et al. Structures of human Golgi-resident glutaminyl cyclase and its complexes with inhibitors reveal a large loop movement upon inhibitor binding. J Biol Chem. 2011;286(14):12439-12449