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 No.: 162203-65-8
- Formule: C19H25N3O4
- Masse moléculaire:359.42
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
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.
Chemical Information
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CAS No. 162203-65-8
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Masse moléculaire 359.42
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Formule C19H25N3O4
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SMILES
O=C(N1[C@H](C(N2[C@H](C(CO)=O)CCC2)=O)CCC1)NCC3=CC=CC=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JTP-4819 Related Classifications
HY-15112 Related Classifications
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