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KYP 2047

Cat. No. 6272 Submit a Review Datasheet / COA / SDS
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Description: High affinity prolyl oligopeptidase inhibitor; anti-angiogenic, neuroprotective and brain penetrant
Chemical Name: (2S)-1-[[(2S)-1-(1-Oxo-4-phenylbutyl)-2-pyrrolidinyl]carbonyl]-2-pyrrolidinecarbonitrile
Purity: ≥98% (HPLC)
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Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity 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.

Technical Data for KYP 2047

M. Wt 339.44
Formula C20H25N3O2
Storage Store at -20°C
Purity ≥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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

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

Solubility Data for KYP 2047

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 33.94 100
ethanol 16.97 50

Preparing Stock Solutions for KYP 2047

The following data is based on the product molecular weight 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 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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References for KYP 2047

References are publications that support the biological activity of the product.

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

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Citations for KYP 2047

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