THPP-1
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- CAS号:
- 1257051-63-0
- 英文名:
- THPP-1
- 英文别名:
- 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-
- 中文名:
- THPP-1
- 中文别名:
- 化合物THPP-1
- CBNumber:
- CB06127943
- 分子式:
- C23H21ClN6O3
- 分子量:
- 464.9
- MOL File:
- 1257051-63-0.mol
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THPP-1化学性质
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密度:
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1.45±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 31.25 mg/mL (67.22 mM)
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形态:
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A solid
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酸度系数(pKa):
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4.70±0.30(Predicted)
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颜色:
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Off-white to light yellow
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THPP-1性质、用途与生产工艺
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。
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.
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Animal Model:
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Male Wistar Hannover rats ranging from 200 to 300 g.
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Dosage:
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0.1-1.0 mg/kg.
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Administration:
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P.O.
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Result:
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Showed novel object recognition.
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Animal Model:
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Eleven monkeyswere surgically implanted with subcutaneous telemetric devices to permit the simultaneous recording of electrocorticogram (ECoG), electrooculogram (EOG), and electromyogram (EMG) activit
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Dosage:
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1, 3, 10 mg/kg.
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Administration:
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P.O.
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Result:
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Significantly attenuated the stimulant effects in SIMA.
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Animal Model:
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Male Wistar Hannover rats ranging from 200 to 300 g.
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Dosage:
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1-30 mg/kg.
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Administration:
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P.O. (10% Tween 80/90% water) 2 h prior to tissue collection (
Pharmacokinetic Analysis
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Result:
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Dose-dependently increases phosphorylation of GluR1 S845.
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THPP-1
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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| 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 |
1257051-63-0, THPP-1 相关搜索:
- 化合物THPP-1
- 1257051-63-0
- 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-
- PDE10A,SIMA,object,THPP 1,recognition,Phosphodiesterase (PDE),Inhibitor,inhibit,novel,THPP-1,THPP1
- THPP-1