[CAS NO. 162203-65-8] JTP-4819
PRODUCTS SPECIFICATIONS [162203-65-8]
DESCRIPTION [162203-65-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 359.42 |
| Molecular Formula | C19H25N3O4 |
| SMILES | O=C(N1[C@H](C(N2[C@H](C(CO)=O)CCC2)=O)CCC1)NCC3=CC=CC=C3 |
Summary
JTP-4819 is a potent and specific inhibitor of prolyl endopeptidase ( PREP ) with IC 50 s 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 IC
50
s of 9.6, 13.9, 10.7, 14.0, 4.5, 7.6 and 10.6 nM, respectively
[1]
.
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 |
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.