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KYP 2047

Cat. No. 6272 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： High affinity prolyl oligopeptidase inhibitor; anti-angiogenic, neuroprotective and brain penetrant
化学名： (2S)-1-[[(2S)-1-(1-Oxo-4-phenylbutyl)-2-pyrrolidinyl]carbonyl]-2-pyrrolidinecarbonitrile
纯度： ≥98% (HPLC)
说明书
引用文献
评论
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for KYP 2047

KYP 2047 is a 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. It reduces tau aggregation in tau-transfected HEK-293 cells and N2A cells as well as in human iPSC-derived neurons from patients with frontotemporal dementia. In vivo, treatment with KYP 2047 of transgenic mice with tauopathy, reduces tau aggregation in the brain and cerebrospinal fluid and slows cognitive decline. Anti-angiogenic and neuroprotective. Brain penetrant.

技术数据 for KYP 2047

分子量 339.44
公式 C20H25N3O2
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 796874-99-2
PubChem ID 11198569
InChI Key SPXFAUXQZWJGCJ-ROUUACIJSA-N
Smiles O=C(N1CCC[C@H]1C#N)[C@@H]2CCCN2C(CCCC3=CC=CC=C3)=O

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for KYP 2047

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 33.94 100
ethanol 16.97 50

制备储备液 for KYP 2047

以下数据基于产品分子量 339.44。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.95 mL 14.73 mL 29.46 mL
5 mM 0.59 mL 2.95 mL 5.89 mL
10 mM 0.29 mL 1.47 mL 2.95 mL
50 mM 0.06 mL 0.29 mL 0.59 mL

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参考文献 for KYP 2047

参考文献是支持产品生物活性的出版物。

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

Eteläinen et al (2023) A prolyl oligopeptidase inhibitor reduces tau pathology in cellular models and in mice with tauopathy. Sci.Transl.Med. 15 PMID: 37043557

If you know of a relevant reference for KYP 2047, please let us know.

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关键词: KYP 2047, KYP 2047 supplier, KYP2047, high, affinity, prolyl, oligopeptidase, inhibitors, inhibits, PREP, α-synuclein, alpha-synuclein, a-synuclein, AcSDKP, anti-angiogenic, neuroprotective, Parkinsons, disease, PEP, PE, Other, Proteases, 6272, Tocris Bioscience

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