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

GSK256066 

Cat. No.: HY-10469 Purity: 98.83%
Handling Instructions

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.

For research use only. We do not sell to patients.

GSK256066 Chemical Structure

GSK256066 Chemical Structure

CAS No. : 801312-28-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 330 In-stock
Estimated Time of Arrival: December 31
50 mg USD 960 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1210 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of GSK256066:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)

In Vitro

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].

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

In Vivo

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].

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.
Clinical Trial
Molecular Weight

518.58

Formula

C₂₇H₂₆N₄O₅S

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : 6.4 mg/mL (12.34 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

GSK256066GSK 256066GSK-256066Phosphodiesterase (PDE)high-affinityphosphodiesterase4PDEPDE4BchronicobstructivepulmonarydiseaseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
GSK256066
Cat. No.:
HY-10469
Quantity:
MCE Japan Authorized Agent: