THPP-1
目录号 : KM6024 CAS No. : 1257051-63-0 纯度 : 98%

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。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
25mg
In-stock
50mg
In-stock
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

Other Forms of Rapamycin:

KKL Med 的所有产品和服务仅用于科学研究,不能被用于人体,兽医,我们也不向个人提供产品和服务。
生物活性

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

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.
分子量
464.90
CAS号
1257051-63-0
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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。

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
在线客服
咨询热线
400-881-9290
关注微信公众号