THPP-1|cas:1257051-63-0|西域试剂

THPP-1,98.75%

产品编号：Bellancom-117604| CAS NO：1257051-63-0| 分子式：C₂₃H₂₁ClN₆O₃| 分子量：464.90

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-117604	￥900.00	杭州北京（现货）
Bellancom-117604	￥1500.00	杭州北京（现货）
Bellancom-117604	￥3200.00	杭州北京（现货）
Bellancom-117604	￥5400.00	杭州北京（现货）
Bellancom-117604	￥9400.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

THPP-1

产品介绍

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 K_i 值分别为 1 nM 和 1.3 nM。THPP-1 具有良好的药理学特性。

生物活性

THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with K_i values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species.

体外研究

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.

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

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.

体内研究

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

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 31.25 mg/mL (67.22 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1510 mL	10.7550 mL	21.5100 mL
5 mM	0.4302 mL	2.1510 mL	4.3020 mL
10 mM	0.2151 mL	1.0755 mL	2.1510 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式