PBD-150

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Chemical Structure| 790663-33-1 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 :

DMSO: 120 mg/mL(374.52 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
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