1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. GSK356278

GSK356278 

Cat. No.: HY-106003
Handling Instructions

GSK356278 is a potent, selective, orally bioavailable and brain-penetrant inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively. GSK356278 has anti-inflammatory activity, and exhibits anxiolytic and cognition-enhancing effects.

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

GSK356278 Chemical Structure

GSK356278 Chemical Structure

CAS No. : 720704-34-7

Size Price Stock Quantity
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK356278 is a potent, selective, orally bioavailable and brain-penetrant inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively. GSK356278 has anti-inflammatory activity, and exhibits anxiolytic and cognition-enhancing effects[1].

IC50 & Target[1]

PDE4A

8.6 (pIC50)

PDE4B

8.8 (pIC50)

PDE4D

8.7 (pIC50)

In Vitro

GSK356278 competes with [3H]rolipram for the high affinity rolipram binding site (HARBS) with a pKi of 8.6 in a competitive filtration-binding assay to the recombinant human PDE4B2B enzyme expressed in yeast membranes[1].
GSK356278 bounds to the HARBS in rats, mice, marmosets, and ferrets with pKis of 7.9, 7.8, 8.4, and 8.5, respectively[1].
GSK356278 inhibits LPS-induced release of TNF-α in human whole blood, with a pIC50 of 7.6[1].

In Vivo

GSK356278 (0.003-30 mg/kg; p.o.) shows anti-inflammatory activity in rodents at exposures that does not induce pica feeding[1].
GSK356278 (0.1-0.1 mg/kg; p.o.) demonstrates efficacy in a nonhuman primate model of anxiety at exposures that do not induce emesis[1].
GSK356278 (4 doses at 0.03, 0.1, 0.3, and 1.0 mg/kg for 6 weeks; p.o.) enhances performance in a nonhuman primate object retrieval test[1]. GSK356278 exhibits oral bioavailability (rat 91%, monkey 23%) and Cmax (rat 205, monkey 41 nM) following oral administration (rat 1, monkey 0.2 mg/kg)[1].
GSK356278 exhibits terminal elimination half-lives (rat 2.2, monkey 1.5 h) due to moderate blood clearance (rat 40, monkey 16 mL/min/kg) combined with volumes of distribution (rat 6.3, monkey 2.1 L/kg) following intravenous administration (rat 1, monkey 0.2 mg/kg)[1].

Animal Model: Male Lewis rats (320-400 g) are treated with lipopolysaccharide (LPS)[1]
Dosage: 0.003-3 mg/kg
Administration: P.o. administration 30 minutes prior to the LPS challenge
Result: Reduced the level of neutrophilia in a dose-dependent manner, with an ED50 of 0.09 mg/kg.
Animal Model: Male CD rats[1]
Dosage: 1 mg/kg (Pharmacokinetic Analysis)
Administration: I.v. and p.o. administration
Result: Oral bioavailability (91%), Cmax (205 nM), T1/2 (2.2 h).
Molecular Weight

439.53

Formula

C₂₁H₂₅N₇O₂S

CAS No.

720704-34-7

SMILES

CCN1C2=NC=C(C3=NN=C(CC4=C(C)N=C(C)S4)O3)C(NC5CCOCC5)=C2C=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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:

GSK356278GSK 356278GSK-356278Phosphodiesterase (PDE)phosphodiesterasePDE4anti-inflammatoryanxiolyticcognitionInhibitorinhibitorinhibit

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:
GSK356278
Cat. No.:
HY-106003
Quantity:
MCE Japan Authorized Agent: