2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. PDE2/PDE10-IN-1

PDE2/PDE10-IN-1 是一种磷酸二酯酶 PDE2 和 PDE10 抑制剂，IC50 分别为 29 和 480 nM。

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PDE2/PDE10-IN-1 Chemical Structure

PDE2/PDE10-IN-1 Chemical Structure

CAS No. : 1426833-08-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4620
In-stock
1 mg ￥1909
In-stock
5 mg ￥4200
In-stock
10 mg 现货 询价
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

PDE2/PDE10-IN-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

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

PDE2/PDE10-IN-1 is a phosphodiesterase 2 (PDE2) and PDE10 inhibitor with IC50s of 29 and 480 nM, respectively.

IC50 & Target

hPDE2A

29 nM (IC50)

rPDE10A

480 nM (IC50)

hPDE11A

6920 nM (IC50)

hPDE4D

5890 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
6920 nM
Compound: 6
Inhibition of full length human PDE11A4 expressed in HEK cells by scintillation proximity assay
Inhibition of full length human PDE11A4 expressed in HEK cells by scintillation proximity assay
[PMID: 25815146]
Sf9 IC50
> 10000 nM
Compound: 6
Inhibition of 6-His-tagged human recombinant PDE5A3 expressed in Sf9 cells by scintillation proximity assay
Inhibition of 6-His-tagged human recombinant PDE5A3 expressed in Sf9 cells by scintillation proximity assay
[PMID: 25815146]
Sf9 IC50
> 10000 nM
Compound: 6
Inhibition of 6-His-tagged human recombinant PDE7A1 expressed in Sf9 cells by scintillation proximity assay
Inhibition of 6-His-tagged human recombinant PDE7A1 expressed in Sf9 cells by scintillation proximity assay
[PMID: 25815146]
Sf9 IC50
> 10000 nM
Compound: 6
Inhibition of 6-His-tagged human recombinant PDE9A1 expressed in Sf9 cells by scintillation proximity assay
Inhibition of 6-His-tagged human recombinant PDE9A1 expressed in Sf9 cells by scintillation proximity assay
[PMID: 25815146]
Sf9 IC50
29 nM
Compound: 6
Inhibition of 6-His-tagged human recombinant PDE2A expressed in Sf9 cells using [3H]cGMP incubated for 40 mins by scintillation proximity assay
Inhibition of 6-His-tagged human recombinant PDE2A expressed in Sf9 cells using [3H]cGMP incubated for 40 mins by scintillation proximity assay
[PMID: 25815146]
Sf9 IC50
480 nM
Compound: 6
Inhibition of 6-His-tagged rat recombinant PDE10A expressed in Sf9 cells using [3H]cAMP incubated for 60 mins by scintillation proximity assay
Inhibition of 6-His-tagged rat recombinant PDE10A expressed in Sf9 cells using [3H]cAMP incubated for 60 mins by scintillation proximity assay
[PMID: 25815146]
Sf9 IC50
5890 nM
Compound: 6
Inhibition of 6-His-tagged human recombinant PDE4D3 expressed in Sf9 cells by scintillation proximity assay
Inhibition of 6-His-tagged human recombinant PDE4D3 expressed in Sf9 cells by scintillation proximity assay
[PMID: 25815146]
体外研究
(In Vitro)

PDE2/PDE10-IN-1 (Compound 6) inhibits PDE2 and PDE10, respectively, with an IC50 value of 29 and 480 nM. PDE2/PDE10-IN-1 also inhibits PDE11A and PDE4D with IC50s of 6920 nM and 5890 nM, respectively. In addition PDE2/PDE10-IN-1 does not show significant inhibition of a panel of CYP450 enzymes (CYP1A2, 2C9, 2D6, 2C19, and 3A4). PDE2/PDE10-IN-1 is also inactive up to a concentration of 125 μg/mL in a bacterial mutagenicity assay[1].

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

PDE2/PDE10-IN-1 相关抗体:
体内研究
(In Vivo)

The PK properties of PDE2/PDE10-IN-1 are studied in rats after 2.5 mg/kg i.v. and 10 mg/kg p.o. administration. After i.v. administration, a rapid clearance is observed (t1/2=0.47 h), which is not expected based on the in vitro metabolic stability in rat liver microsomes (rLMs). Interestingly, PDE2/PDE10-IN-1 shows much slower clearance after p.o. administration (t1/2=2.36 h), resulting in good bioavailability and a maximum plasma concentration (Cmax) of 997 ng/mL. PDE2/PDE10-IN-1 is assessed for its potential to cross the blood–brain barrier in rats after 10 mg/kg s.c. administration. PDE2/PDE10-IN-1 shows good formulatability with 10 to 20% HPβCD at pH>3.5. The brain concentration for PDE2/PDE10-IN-1 after 1 h administration is in the range of 370-895 ng/g with high brain free fractions and brain/plasma ratios. More specifically, PDE2/PDE10-IN-1, which is orally bioavailable, occupies PDE2 with an ED50 of 21 mg/kg[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

295.73

Formula

C15H10ClN5
CAS 号
性状

固体

颜色

Off-white to brown

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
细胞实验： 

DMSO 中的溶解度 : 12.5 mg/mL (42.27 mM; 超声助溶 (<60°C); 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 3.3815 mL 16.9073 mL 33.8146 mL
5 mM 0.6763 mL 3.3815 mL 6.7629 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, 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。

  • 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

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (4.23 mM); 澄清溶液

    此方案可获得 ≥ 1.25 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.25 mg/mL (4.23 mM); 澄清溶液

    此方案可获得 ≥ 1.25 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
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
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.88%

COA (276 KB) HNMR (101 KB) LCMS (246 KB)

产品使用指南 (1538 KB)
参考文献
Animal Administration
[1]

Rats[1]
Male Sprague-Dawley rats are fed with PDE2/PDE10-IN-1 (i.v., 2.5 mg/kg; p.o., 10 mg/kg). After administration, the clearance is observed.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

PDE2/PDE10-IN-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, 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3815 mL 16.9073 mL 33.8146 mL 84.5366 mL
5 mM 0.6763 mL 3.3815 mL 6.7629 mL 16.9073 mL
10 mM 0.3381 mL 1.6907 mL 3.3815 mL 8.4537 mL
15 mM 0.2254 mL 1.1272 mL 2.2543 mL 5.6358 mL
20 mM 0.1691 mL 0.8454 mL 1.6907 mL 4.2268 mL
25 mM 0.1353 mL 0.6763 mL 1.3526 mL 3.3815 mL
30 mM 0.1127 mL 0.5636 mL 1.1272 mL 2.8179 mL
40 mM 0.0845 mL 0.4227 mL 0.8454 mL 2.1134 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:

PDE2/PDE10-IN-11426833-08-0Phosphodiesterase (PDE)Inhibitorinhibitorinhibit

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