(2S)-N-benzyl-2-[(2S)-2-(2-hydroxyacetyl)pyrrolidine-1-carbonyl]pyrrolidine-1-carboxamide
![(2S)-N-benzyl-2-[(2S)-2-(2-hydroxyacetyl)pyrrolidine-1-carbonyl]pyrrolidine-1-carboxamide Structure](CAS/GIF/162203-65-8.gif)
- CAS No.
- 162203-65-8
- Chemical Name:
- (2S)-N-benzyl-2-[(2S)-2-(2-hydroxyacetyl)pyrrolidine-1-carbonyl]pyrrolidine-1-carboxamide
- Synonyms
- (S)-N-Benzyl-2-((S)-2-(2-hydroxyacetyl)pyrrolidine-1-carbonyl)pyrrolidine-1-carboxamide;JTP 4819;(2S)-N-benzyl-2-[(2S)-2-(2-hydroxyacetyl)pyrrolidine-1-carbonyl]pyrrolidine-1-carboxamide;1-Pyrrolidinecarboxamide, 2-[[(2S)-2-(hydroxyacetyl)-1-pyrrolidinyl]carbonyl]-N-(phenylmethyl)-, (2S)-
- CBNumber:
- CB11456595
- Molecular Formula:
- C19H25N3O4
- Molecular Weight:
- 359.42
- MDL Number:
- MOL File:
- 162203-65-8.mol
- MSDS File:
- SDS
(2S)-N-benzyl-2-[(2S)-2-(2-hydroxyacetyl)pyrrolidine-1-carbonyl]pyrrolidine-1-carboxamide Properties
| Boiling point | 673.5±55.0 °C(Predicted) |
|---|---|
| Density | 1.300±0.06 g/cm3(Predicted) |
| pka | 12.91±0.10(Predicted) |
| FDA UNII | ASG803L8RD |
(2S)-N-benzyl-2-[(2S)-2-(2-hydroxyacetyl)pyrrolidine-1-carbonyl]pyrrolidine-1-carboxamide Chemical Properties,Uses,Production
Uses
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 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 |
References
[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. PMID:7562510
(2S)-N-benzyl-2-[(2S)-2-(2-hydroxyacetyl)pyrrolidine-1-carbonyl]pyrrolidine-1-carboxamide Preparation Products And Raw materials
Raw materials
Preparation Products
(2S)-N-benzyl-2-[(2S)-2-(2-hydroxyacetyl)pyrrolidine-1-carbonyl]pyrrolidine-1-carboxamide Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| BOC Sciences | 1-631-485-4226; 16314854226 | info@bocsci.com | United States | 9920 | 65 |
| Shanghai Synchem Pharma Co., ltd | 21-619849051-1 18521059765 | synchempharma@aliyun.com | China | 4988 | 55 |
| Nextpeptide Inc | +86-0571-81612335 +8613336028439 | sales@nextpeptide.com | China | 19904 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 29874 | 58 |
| TargetMol Chemicals Inc. | 13564774135 | marketing@targetmol.com | United States | 19950 | 58 |
| Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49709 | 58 |
| Supplier | Advantage |
|---|---|
| BOC Sciences | 65 |
| Shanghai Synchem Pharma Co., ltd | 55 |
| Nextpeptide Inc | 58 |
| TargetMol Chemicals Inc. | 58 |
| TargetMol Chemicals Inc. | 58 |
| Hangzhou MolCore BioPharmatech Co.,Ltd. | 58 |
