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Art. -Nr.: HY-15112

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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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CAS. Nr.: 162203-65-8
Formel: C₁₉H₂₅N₃O₄
Molecular Weight:359.42

Speicherung:

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

Data Sheet (273 KB)

JTP-4819 Chemical Structure

CAS. Nr.: 162203-65-8

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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]

	AUC_{0-300 min} (μg·min)	C_max (μM)	Brain/blood ratio	t_1/2β (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.

Chemical Information

CAS. Nr. 162203-65-8
Molecular Weight 359.42
Formel C₁₉H₂₅N₃O₄
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Toide K, et al. JTP-4819: a novel prolyl endopeptidase inhibitor with potential as a cognitive enhancer. J Pharmacol Exp Ther. 1995 Sep;274(3):1370-8. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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