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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 |
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溶解度 : | - | |
动物实验配方: |
生物活性 | |||
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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 | |||
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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 |
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