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

GSK356278 

Cat. No.: HY-106003 Purity: 99.89%
COA 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

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10 mg USD 110 In-stock
50 mg USD 390 In-stock
100 mg USD 620 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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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].

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

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

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).
Clinical Trial
Molecular Weight

439.53

Appearance

Solid

Formula

C21H25N7O2S
CAS No.
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

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
In Vitro: 

DMSO : 2.5 mg/mL (5.69 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2752 mL 11.3758 mL 22.7516 mL
5 mM 0.4550 mL 2.2752 mL 4.5503 mL
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.25 mg/mL (2.84 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.25 mg/mL (2.84 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.25 mg/mL (2.84 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.89%

COA (249 KB) HNMR (270 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References
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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.

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Keywords:

GSK356278720704-34-7GSK 356278GSK-356278Phosphodiesterase (PDE)phosphodiesterasePDE4anti-inflammatoryanxiolyticcognitionInhibitorinhibitorinhibit

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