2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. GSK256066

GSK256066 is a selective and high-affinity phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 is developed for the research of chronic obstructive pulmonary disease.

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GSK256066

GSK256066 構造式

CAS 番号 : 801312-28-7

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 108 在庫あり
Solution
10 mM * 1 mL in DMSO USD 108 在庫あり
Solid
5 mg $95 在庫あり
10 mg $160 在庫あり
25 mg $320 在庫あり
50 mg $520 在庫あり
100 mg $840 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

This product is a controlled substance and not for sale in your territory.

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Based on 1 publication(s) in Google Scholar

Other Forms of GSK256066:

GSK256066 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

GSK256066 is a selective and high-affinity phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 is developed for the research of chronic obstructive pulmonary disease[1].

IC50 & Target[1]

PDE4

3.2 pM (IC50)

体外実験

GSK256066 is an exceptionally high-affinity inhibitor of PDE4 designed for inhaled administration[1].
? GSK256066 is highly selective for PDE4, with >380,000-fold versus PDE1/2/3/5/6 and >2500-fold against PDE7[1].
? GSK256066 inhibits PDE4 isoforms A-D with equal affinity (PDE4B: pIC50≥ 11.5, PDE4A: pIC50≥11.31, PDE4C: pIC50≥11.42, PDE4D: pIC50≥11.94)[1].
? GSK256066 inhibits TNF-α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with IC50 of 0.01 nM[1].

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

GSK256066 関連抗体
体内実験

GSK256066 (10 μg/kg; i.t.) causes significant inhibition of LPS-induced pulmonary neutrophilia[2].
? GSK256066 also inhibits LPS-induced increases in exhaled nitric oxide (ED50=92 μg/kg)[2].
? GSK256066 inhibits pulmonary eosinophilia in rats exposed to ovalbumin (ED50=0.4 μg/kg)[2].

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

Animal Model: Male Brown Norway rats (180-200 g)[2]
Dosage: 10 μg/kg
Administration: Intratracheal injection; before (36 hours, 24 hours, 18 hours, 12 hours, 6 hours, and 2 hours) and after (0 hour, 2 hours) LPS challenge
Result: Inhibited the LPS-induced pulmonary neutrophilia.
臨床実験
分子量

518.58

分子式

C27H26N4O5S
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N)C1=C(C2=CC(S(=O)(C3=CC=CC(C(N(C)C)=O)=C3)=O)=CC(C)=C2N=C1)NC4=CC=CC(OC)=C4
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 : 25 mg/mL (48.21 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 1.9283 mL 9.6417 mL 19.2834 mL
5 mM 0.3857 mL 1.9283 mL 3.8567 mL
10 mM 0.1928 mL 0.9642 mL 1.9283 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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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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Calculation results:
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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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9283 mL 9.6417 mL 19.2834 mL 48.2086 mL
5 mM 0.3857 mL 1.9283 mL 3.8567 mL 9.6417 mL
10 mM 0.1928 mL 0.9642 mL 1.9283 mL 4.8209 mL
15 mM 0.1286 mL 0.6428 mL 1.2856 mL 3.2139 mL
20 mM 0.0964 mL 0.4821 mL 0.9642 mL 2.4104 mL
25 mM 0.0771 mL 0.3857 mL 0.7713 mL 1.9283 mL
30 mM 0.0643 mL 0.3214 mL 0.6428 mL 1.6070 mL
40 mM 0.0482 mL 0.2410 mL 0.4821 mL 1.2052 mL
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GSK256066 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:

GSK256066801312-28-7GSK 256066GSK-256066Phosphodiesterase (PDE)high-affinityphosphodiesterase4PDEPDE4BchronicobstructivepulmonarydiseaseInhibitorinhibitorinhibit

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製品名:
GSK256066
製品番号:
HY-10469
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