KYP 2047

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Cat.No. 6272 - KYP 2047 | C20H25N3O2 | CAS No. 796874-99-2
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)
Datasheet
Citations (1)
Reviews
Literature

Biological Activity

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.

Technical Data

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

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

Preparing Stock Solutions

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.

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

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


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1 Citation for KYP 2047

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