1257051-63-0
中文名称
THPP-1
英文名称
THPP-1
CAS
1257051-63-0
分子式
C23H21ClN6O3
分子量
464.9
MOL 文件
1257051-63-0.mol
更新日期
2023/03/20 15:41:27
1257051-63-0 结构式
物理化学性质
密度1.45±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO: 31.25 mg/mL (67.22 mM)
酸度系数(pKa)4.70±0.30(Predicted)
形态固体
颜色Off-white to light yellow
THPP-1价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/11/08 | HY-117604 | THPP-1 THPP-1 | 1257051-63-0 | 5mg | 900元 |
| 2024/11/08 | HY-117604 | THPP-1 THPP-1 | 1257051-63-0 | 10mM * 1mLin DMSO | 921元 |
| 2024/11/08 | HY-117604 | THPP-1 THPP-1 | 1257051-63-0 | 10mg | 1500元 |
常见问题列表
生物活性
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。靶点
IC50: 1-1.3 nM (PDE10A).
体内研究
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. |