GSK-356278 | CAS#720704-34-7 | PDE 4 Inhibitor

MedKoo Cat#: 525224 | Name: GSK-356278

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

GSK-356278 is a potent, selective, brain-penetrant phosphodiesterase 4 inhibitor that demonstrates anxiolytic and cognition-enhancing effects. GSK-356278 has the ability to elevate cAMP in various cell types of the central nervous system.

Chemical Structure

GSK-356278

CAS#720704-34-7

Theoretical Analysis

MedKoo Cat#: 525224

Name: GSK-356278

CAS#: 720704-34-7

Chemical Formula: C21H25N7O2S

Exact Mass: 439.1790

Molecular Weight: 439.54

Elemental Analysis: C, 57.38; H, 5.73; N, 22.31; O, 7.28; S, 7.30

Price and Availability

Size	Price	Availability
10mg	USD 350.00	2 Weeks
25mg	USD 550.00	2 Weeks
50mg	USD 850.00	2 Weeks
100mg	USD 1,250.00	2 Weeks

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Related CAS #

No Data

Synonym

GSK-356278; GSK356278; GSK 356278;

IUPAC/Chemical Name

1H-Pyrazolo(3,4-b)pyridin-4-amine, 5-(5-((2,4-dimethyl-5-thiazolyl)methyl)-1,3,4-oxadiazol-2-yl)-1-ethyl-n-(tetrahydro-2H-pyran-4-yl)-

InChi Key

AWDJJMXJUOHGLC-UHFFFAOYSA-N

InChi Code

InChI=1S/C21H25N7O2S/c1-4-28-20-15(11-23-28)19(25-14-5-7-29-8-6-14)16(10-22-20)21-27-26-18(30-21)9-17-12(2)24-13(3)31-17/h10-11,14H,4-9H2,1-3H3,(H,22,25)

SMILES Code

CCN1N=CC2=C(NC3CCOCC3)C(C4=NN=C(CC5=C(C)N=C(C)S5)O4)=CN=C21

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

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.

In vitro activity:

GSK356278 inhibited PDE4B enzyme activity with a pIC50 of 8.8 and bound to the high-affinity rolipram binding site with a pIC50 of 8.6. Reference: J Pharmacol Exp Ther. 2014 Jul;350(1):153-63. https://pubmed.ncbi.nlm.nih.gov/24784567/

In vivo activity:

In preclinical models, the therapeutic index as defined in a rodent lung inflammation model versus rat pica feeding was >150 compared with 0.5 and 6.4 for rolipram and roflumilast, respectively. In a model of anxiety in common marmosets, the therapeutic index for GSK356278 was >10 versus <1 for rolipram. Reference: J Pharmacol Exp Ther. 2014 Jul;350(1):153-63. https://pubmed.ncbi.nlm.nih.gov/24784567/

	Solvent	mg/mL	mM
Solubility
	DMSO	25.0	56.88

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 439.54 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Rutter AR, Poffe A, Cavallini P, Davis TG, Schneck J, Negri M, Vicentini E, Montanari D, Arban R, Gray FA, Davies CH, Wren PB. GSK356278, a potent, selective, brain-penetrant phosphodiesterase 4 inhibitor that demonstrates anxiolytic and cognition-enhancing effects without inducing side effects in preclinical species. J Pharmacol Exp Ther. 2014 Jul;350(1):153-63. doi: 10.1124/jpet.114.214155. Epub 2014 Apr 30. PMID: 24784567.

In vitro protocol:

In vivo protocol:

1: Rutter AR, Poffe A, Cavallini P, Davis TG, Schneck J, Negri M, Vicentini E, Montanari D, Arban R, Gray FA, Davies CH, Wren PB. GSK356278, a potent, selective, brain-penetrant phosphodiesterase 4 inhibitor that demonstrates anxiolytic and cognition-enhancing effects without inducing side effects in preclinical species. J Pharmacol Exp Ther. 2014 Jul;350(1):153-63. doi: 10.1124/jpet.114.214155. Epub 2014 Apr 30. PubMed PMID: 24784567.