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KYP-2047

Cat. No. M8258
KYP-2047 Structure
Synonym:

KYP2047

Size Price Availability Quantity
5mg USD 135  USD135 In stock
10mg USD 210  USD210 In stock
25mg USD 360  USD360 In stock
50mg USD 540  USD540 In stock
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Quality Control & Documentation
Biological Activity

KYP-2047 is a potent and BBB-penetrating prolyl-oligopeptidase (POP) inhibitor, with an Ki value of 0.023 nM. KYP-2047 reduces glioblastoma proliferation through angiogenesis and apoptosis modulation. KYP-2047 clears the α-synuclein aggregates induced by oxidative stress in the neuronal cells. α-synuclein is the main component of Lewy bodies in Parkinson′s disease that cause neuronal cell death and dementia.

KYP-2047 (0-100 μM) decreases U-87, U-138 and A-172 cell viability in a concentration-dependent manner. KYP-2047 (0-100 μM) increases the pro-apoptotic protein Bax, p53 and caspase-3 expression whereas reduces Bcl-2 expression, and reduced significantly TGF-β expression.

KYP-2047 (0-5 mg/kg) significantly reduces tumor mass and neutrophil infiltration.

Chemical Information
Molecular Weight 339.43
Formula C20H25N3O2
CAS Number 796874-99-2
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Sarah Adriana Scuderi, et al. Beneficial effect of KYP-2047, a propyl-oligopeptidase inhibitor, on oral squamous cell carcinoma

[2] Sarah Adriana Scuderi, et al. KYP-2047, an Inhibitor of Prolyl-Oligopeptidase, Reduces GlioBlastoma Proliferation through Angiogenesis and Apoptosis Modulation

[3] Aaro J Jalkanen, et al. KYP-2047 penetrates mouse brain and effectively inhibits mouse prolyl oligopeptidase

[4] T T Myhnen, et al. A prolyl oligopeptidase inhibitor, KYP-2047, reduces α-synuclein protein levels and aggregates in cellular and animal models of Parkinson's disease

[5] Aaro J Jalkanen, et al. Brain pharmacokinetics of two prolyl oligopeptidase inhibitors, JTP-4819 and KYP-2047, in the rat

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