1. Metabolic Enzyme/Protease
  2. Prolyl Endopeptidase (PREP)
  3. JTP-4819

JTP-4819 是脯氨酸肽酶 (PREP) 的强效、特异性抑制剂,IC50 为 0.83 nM (在大鼠脑上清中) 和 5.43 nM (在脑膜炎黄杆菌中)。JTP-4819 具有血脑穿透性,能够改善受 Scopolamine (HY-N2096) 诱导的健忘大鼠的记忆停留时间。

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JTP-4819 Chemical Structure

JTP-4819 Chemical Structure

CAS No. : 162203-65-8

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(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]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

359.42

Formula

C19H25N3O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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JTP-4819
目录号:
HY-15112
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