1. Metabolic Enzyme/Protease
  2. Prolyl Endopeptidase (PREP)
  3. JTP-4819

JTP-4819 is a potent and specific inhibitor of prolyl endopeptidase (PREP) with IC50s of 0.83 nM (in rat brain supernatant) and 5.43 nM (in Flavobacterium meningosepticum). JTP-4819 has blood-brain penetration, also improves the retention time of amnesia rats induced by Scopolamine (HY-N2096).

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JTP-4819 Chemical Structure

JTP-4819 Chemical Structure

CAS No. : 162203-65-8

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Description

JTP-4819 is a potent and specific inhibitor of prolyl endopeptidase (PREP) with IC50s of 0.83 nM (in rat brain supernatant) and 5.43 nM (in Flavobacterium meningosepticum). JTP-4819 has blood-brain penetration, also improves the retention time of amnesia rats induced by Scopolamine (HY-N2096)[1][2].

In Vitro

JTP-4819 inhibits the degradation of substance P, arginine-vasopressin, thyrotropin-releasing hormone, neurotensin, oxytocin, bradykinin, and angiotensin II by purified PREP with IC50s of 9.6, 13.9, 10.7, 14.0, 4.5, 7.6 and 10.6 nM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

JTP-4819 (1 and 3 mg/kg 1 hr before acquisition or at 3 and 10 mg/kg 1 hr before; p.o.) significantly prolonged the retention time in the one-trial passive avoidance test in rats with Scopolamine (HY-N2096)-induced amnesia[1].
JTP-4819 (1 mg/kg and 3 mg/kg; p.o.; single dose) causes a significant increase in ACh release in the frontal cortex and hippocampus of young rats, as well as in both brain regions of aged rats at higher dose[1].
JTP-4819 combinded with substance P, arginine-vasopressin or thyrotropin-releasing hormone, improves the retention time of rats with scopolamine-induced amnesia[1].

Brain pharmacokinetics in rats[2]

AUC0-300 min (μg·min) Cmax (μM) Brain/blood ratio t1/2β (min)
Unblound concentrations
Blood 1947 16.7 84
Cortex 206 1.78 0.13 77
Hippocampus 128 1.05 0.09 105
Striatum 178 1.26 0.10 128
Total tissue concentrations
Plasma 4230 78.6 130
Brain 145 1.47 0.034 120

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

359.42

Formula

C19H25N3O4

CAS No.
SMILES

O=C(N1[C@H](C(N2[C@H](C(CO)=O)CCC2)=O)CCC1)NCC3=CC=CC=C3

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Product Name:
JTP-4819
Cat. No.:
HY-15112
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