1257051-63-0
中文名稱
THPP-1
英文名稱
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 結(jié)構(gòu)式
物理化學性質(zhì)
密度1.45±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO: 31.25 mg/mL (67.22 mM)
酸度系數(shù)(pKa)4.70±0.30(Predicted)
形態(tài)固體
顏色Off-white to light yellow
THPP-1價格(試劑級)
| 報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
| 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 |
常見問題列表
生物活性
THPP-1 是SGC推薦的一個化學探針， 是有效的、具有口服活性的磷酸二酯酶10A (PDE10A) 的抑制劑，其對人和大鼠的 Ki 值分別為 1 nM 和 1.3 nM。THPP-1 具有良好的藥理學特性。靶點
IC50: 1-1.3 nM (PDE10A).
體內(nèi)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. |