162203-65-8
162203-65-8 structure
- Name: JTP-4819
- Chemical Name: (2S)-N-benzyl-2-[(2S)-2-(2-hydroxyacetyl)pyrrolidine-1-carbonyl]pyrrolidine-1-carboxamide
- CAS Number: 162203-65-8
- Molecular Formula: C19H25N3O4
- Molecular Weight: 359.42000
- Create Date: 2017-10-28 22:54:04
- Modify Date: 2024-02-03 19:51:43
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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].
| Name | (2S)-N-benzyl-2-[(2S)-2-(2-hydroxyacetyl)pyrrolidine-1-carbonyl]pyrrolidine-1-carboxamide |
|---|---|
| Synonyms | Jtp 4819 |
| 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 抑制纯化 PREP 对 P 物质、精氨酸-加压素、促甲状腺激素释放激素、神经紧张素、催产素、缓激肽和血管紧张素II的降解，IC50 分别为 9.6、13.9、10.7、14.0、4.5、7.6 和 10.6 nM[1]。 |
| In Vivo | JTP-4819 (1 mg/kg 和 3 mg/kg, 试验前 1 小时或 3 小时给药；或 10 mg/k，试验前1小时给药；口服) 在 Scopolamine (HY-N2096) 诱导的健忘症大鼠的一次试验被动回避测试中，显著延长了记忆时间[1]。 JTP-4819 (1 mg/kg 和 3 mg/kg; 口服; 单剂量) 导致年轻大鼠额叶皮层和海马体中 ACh 释放显著增加，老年大鼠在高剂量时也会显著增加这两个脑区 ACh 释放[1]。 JTP-4819 联合 P 物质、精氨酸-抗利尿激素或促甲状腺激素释放激素可改善东莨菪碱性遗忘大鼠的记忆保留时间[1]。 在大鼠中试验的脑药代动力学[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 |
| Molecular Formula | C19H25N3O4 |
|---|---|
| Molecular Weight | 359.42000 |
| Exact Mass | 359.18500 |
| PSA | 93.44000 |
| LogP | 0.99320 |
| Vapour Pressure | 4.68E-19mmHg at 25°C |