KYP 2047 是一种有效的 BBB 穿透性脯氨酰寡肽酶 (POP) 抑制剂，Ki 值为 0.023 nM。 KYP 2047 通过血管生成和细胞凋亡调节减少胶质母细胞瘤的增殖。
| Cas No. | 796874-99-2 |
| Canonical SMILES | O=C(N1CCC[C@H]1C#N)[C@@H]2CCCN2C(CCCC3=CC=CC=C3)=O |
| 分子式 | C20H25N3O2 |
| 分子量 | 339.44 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | High affinity prolyl oligopeptidase (POP) inhibitor (Ki = 0.023 nM). Clears α-synuclein aggregates induced by oxidative stress in neuronal cells. Inhibits the formation of AcSDKP from its precursor 43-mer thymosin β4 (Tβ4). Induces angiogenesis via POP inhibition. Anti-angiogenic and neuroprotective. Brain penetrant. Yedlapudi et al (2016) Inhibition of alpha-synuclein aggregation by multifunctional Da agonists assessed by a novel in vitro assay and an in vivo Drosophila synucleinopathy model. Sci Rep. 69 38510 PMID:27917933 |Myöhänen et al (2012) A prolyl oligopeptidase inhibitor, KYP-2047, reduces alpha-synuclein protein levels and aggregates in cellular and animal models of Parkinson's disease. Br.J.Pharmacol. 166 1097 PMID:22233220 |Jalkanen et al (2011) Brain pharmacokinetics of two prolyl oligopeptidase inhibitors, JTP-4819 and KYP-2047, in the rat. Basic Clin.Pharmacol.Toxicol. 109 443 PMID:21707925 |Myöhänen et al (2011) Prolyl oligopeptidase induces angiogenesis both in vitro and in vivo in a novel regulatory manner. Br.J.Pharmacol. 163 1666 PMID:21133893 |Venäläinen et al (2006) Binding kinetics and duration of in vivo action of novel prolyl oligopeptidase inhibitors. Biochem.Pharmacol. 71 683 PMID:16405869 |
