THPP-1
| 中文名称 | THPP-1 |
|---|---|
| 中文同义词 | 化合物THPP-1 |
| 英文名称 | THPP-1 |
| 英文同义词 | THPP-1;PDE10A,SIMA,object,THPP 1,recognition,Phosphodiesterase (PDE),Inhibitor,inhibit,novel,THPP-1,THPP1;Methanone, [2-(6-chloro-3-pyridinyl)-7,8-dihydro-4-(2-methoxyethoxy)pyrido[4,3-d]pyrimidin-6(5H)-yl]imidazo[1,5-a]pyridin-1-yl- |
| CAS号 | 1257051-63-0 |
| 分子式 | C23H21ClN6O3 |
| 分子量 | 464.9 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1257051-63-0.mol |
| 结构式 |  |
THPP-1 性质
| 密度 | 1.45±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | 二甲基亚砜：31.25 mg/mL（67.22 mM） |
| 形态 | 固体 |
| 酸度系数(pKa) | 4.70±0.30(Predicted) |
| 颜色 | 米白色至浅黄色 |
THPP-1 是SGC推荐的一个化学探针， 是有效的、具有口服活性的磷酸二酯酶10A (PDE10A) 的抑制剂，其对人和大鼠的 Ki 值分别为 1 nM 和 1.3 nM。THPP-1 具有良好的药理学特性。
IC50: 1-1.3 nM (PDE10A).
THPP-1 (0.1-1.0 mg/kg, p.o.) shows novel object recognition in rats.
THPP-1 (p.o., 1-30 mg/kg) dose-dependently increases
phosphorylation of GluR1
S845 in the rat striatum whereas the total levels of GluR1 in the striatum are not affected. Administration of THPP-1 also results in an associated increase in the pGluR1/GluR1 ratios at all doses examined in this study.
THPP-1 (1, 3, 10 mg/kg, p.o.) significantly attenuated the stimulant effects in stimulant-induced motor activity (SIMA) in monkey.
| Animal Model: | Male Wistar Hannover rats ranging from 200 to 300 g. |
| Dosage: | 0.1-1.0 mg/kg. |
| Administration: | P.O. |
| Result: | Showed novel object recognition. |
| Animal Model: | Eleven monkeyswere surgically implanted with subcutaneous telemetric devices to permit the simultaneous recording of electrocorticogram (ECoG), electrooculogram (EOG), and electromyogram (EMG) activit |
| Dosage: | 1, 3, 10 mg/kg. |
| Administration: | P.O. |
| Result: | Significantly attenuated the stimulant effects in SIMA. |
| Animal Model: | Male Wistar Hannover rats ranging from 200 to 300 g. |
| Dosage: | 1-30 mg/kg. |
| Administration: | P.O. (10% Tween 80/90% water) 2 h prior to tissue collection ( Pharmacokinetic Analysis ). |
| Result: | Dose-dependently increases phosphorylation of GluR1 S845. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-117604 | THPP-1 THPP-1 | 1257051-63-0 | 5mg | 900元 |
| 2024/04/30 | HY-117604 | THPP-1 THPP-1 | 1257051-63-0 | 10mM * 1mLin DMSO | 921元 |