2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. PF-06445974

PF-06445974, a promising positron emission tomography (PET) lead, has exquisite potency at PDE4B with an IC50 <1 nM. The IC50 values are 36, 4.7 and 17 nM for PDE4D, PDE4A and PDE4C, respectively. PF-06445974 has good selectivity over PDE4D, excellent brain permeability, and a high level of specific binding in the "cold tracer" study.

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PF-06445974

PF-06445974 構造式

CAS 番号 : 2055776-17-3

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 275 在庫あり
Solution
10 mM * 1 mL in DMSO USD 275 在庫あり
Solid
5 mg $250 在庫あり
10 mg $400 在庫あり
25 mg $850 在庫あり
50 mg $1350 在庫あり
100 mg $1950 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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PF-06445974 関連抗体

Top Publications Citing Use of Products

Phosphodiesterase (PDE) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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製品説明

PF-06445974, a promising positron emission tomography (PET) lead, has exquisite potency at PDE4B with an IC50 <1 nM. The IC50 values are 36, 4.7 and 17 nM for PDE4D, PDE4A and PDE4C, respectively. PF-06445974 has good selectivity over PDE4D, excellent brain permeability, and a high level of specific binding in the "cold tracer" study[1].

IC50 & Target[1]

PDE4B

<1 nM (IC50)

PDE4D

36 nM (IC50)

PDE4A

4.7 nM (IC50)

PDE4C

17 nM (IC50)

体外実験

PF-06445974 demonstrates minimal off-target activities in broad-spectrum selectivity panels, with only weak µM activities at PDE10 (IC50=2290 nM), PDE5A (IC50=4640 nM) and GABAA (Ki=3850 nM)[1].

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

PF-06445974 関連抗体
体内実験

PF-06445974 exhibits high central nervous system (CNS) PET MPO score (4.0). PF-06445974 is a promising radiotracer lead for specific binding assessment. Neuropharmacokinetic study in rats (0.1 mg/kg, IV) confirms high brain permeability with a total brain to plasma ratio of 0.76, corresponding to a free brain to plasma ratio of 0.70[1].

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

Animal Model: Twenty-five drug-naive male 129/B6 PDE4D KO mice (25-35 g)[1]
Dosage: 10 µg/kg
Administration: Dosed intravenously at 10 µg/kg in a 5 mL/kg dosing volume
Result: Showed excellent brain uptake and reached peak concentrations at around 20 minutes.
分子量

346.36

分子式

C20H15FN4O
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=CC=C(C=C1F)C2=C(C3=O)N(CCN3C4CC4)C5=CC=CN=C25
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 33.33 mg/mL (96.23 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8872 mL 14.4358 mL 28.8717 mL
5 mM 0.5774 mL 2.8872 mL 5.7743 mL
10 mM 0.2887 mL 1.4436 mL 2.8872 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

一般には略語で表示されます：C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8872 mL 14.4358 mL 28.8717 mL 72.1792 mL
5 mM 0.5774 mL 2.8872 mL 5.7743 mL 14.4358 mL
10 mM 0.2887 mL 1.4436 mL 2.8872 mL 7.2179 mL
15 mM 0.1925 mL 0.9624 mL 1.9248 mL 4.8119 mL
20 mM 0.1444 mL 0.7218 mL 1.4436 mL 3.6090 mL
25 mM 0.1155 mL 0.5774 mL 1.1549 mL 2.8872 mL
30 mM 0.0962 mL 0.4812 mL 0.9624 mL 2.4060 mL
40 mM 0.0722 mL 0.3609 mL 0.7218 mL 1.8045 mL
50 mM 0.0577 mL 0.2887 mL 0.5774 mL 1.4436 mL
60 mM 0.0481 mL 0.2406 mL 0.4812 mL 1.2030 mL
80 mM 0.0361 mL 0.1804 mL 0.3609 mL 0.9022 mL
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PF-06445974 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

PF-064459742055776-17-3PF06445974PF 06445974Phosphodiesterase (PDE)positronemissiontomographyPETPDE4BInhibitorinhibitorinhibit

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製品名:
PF-06445974
製品番号:
HY-119190
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