2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. THPP-1

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。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

THPP-1 Chemical Structure

THPP-1 Chemical Structure

CAS No. : 1257051-63-0

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥921
In-stock
5 mg ￥900
In-stock
10 mg ￥1500
In-stock
25 mg ￥3200
In-stock
50 mg ￥5400
In-stock
100 mg ￥9400
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

THPP-1 相关抗体

Top Publications Citing Use of Products

查看 Phosphodiesterase (PDE) 亚型特异性产品:

查看所有亚型
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target

IC50: 1-1.3 nM (PDE10A)[1].
体内研究
(In Vivo)

THPP-1 (0.1-1.0 mg/kg, p.o.) shows novel object recognition in rats[1].
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[1].
THPP-1 (1, 3, 10 mg/kg, p.o.) significantly attenuated the stimulant effects in stimulant-induced motor activity (SIMA) in monkey[2].

MCE 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[1].
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[1].
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

Formula

C23H21ClN6O3
CAS 号
性状

固体

颜色

Off-white to light yellow

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 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 31.25 mg/mL (67.22 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

THPP-1 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1510 mL 10.7550 mL 21.5100 mL 53.7750 mL
5 mM 0.4302 mL 2.1510 mL 4.3020 mL 10.7550 mL
10 mM 0.2151 mL 1.0755 mL 2.1510 mL 5.3775 mL
15 mM 0.1434 mL 0.7170 mL 1.4340 mL 3.5850 mL
20 mM 0.1076 mL 0.5378 mL 1.0755 mL 2.6888 mL
25 mM 0.0860 mL 0.4302 mL 0.8604 mL 2.1510 mL
30 mM 0.0717 mL 0.3585 mL 0.7170 mL 1.7925 mL
40 mM 0.0538 mL 0.2689 mL 0.5378 mL 1.3444 mL
50 mM 0.0430 mL 0.2151 mL 0.4302 mL 1.0755 mL
60 mM 0.0359 mL 0.1793 mL 0.3585 mL 0.8963 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

THPP-11257051-63-0THPP1THPP 1Phosphodiesterase (PDE)SIMAPDE10AnovelobjectrecognitionInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
THPP-1
目录号：
HY-117604
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z