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Tofimilast

Chemical Structure : Tofimilast

CAS No.: 185954-27-2

Tofimilast (CP-325366, CP325366)

Catalog No.: PC-63090Not For Human Use, Lab Use Only.

Tofimilast (CP-325366) is a potent, selective PDE4 inhibitor with IC50 of 23, 13 and 13 nM for PDE4A, PDE4B, and PDE4D, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Tofimilast (CP-325366) is a potent, selective PDE4 inhibitor with IC50 of 23, 13 and 13 nM for PDE4A, PDE4B, and PDE4D, respectively.
Tofimilast (CP-325366) shows weakly or no inhibition for PDE4C, and no activity for PDE1, PDE2, PDE3, PDE5, PDE6, and PDE7.
Tofimilast (CP-325366) increases cAMP levels in PGE1-stimulated U937 cells with an EC50 of 230 nM, inhibits human monocyte PDE mediated cAMP catabolism with an IC50 of 67 nM and LPS stimulated human monocyte TNFα release with an IC50 of 59 nM.
Tofimilast (CP-325366) shows low oral bioavailability and no emesis-associated behaviors in the ferret emesis model.

Physicochemical Properties

M.Wt 339.461
Formula C18H21N5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

9-Cyclopentyl-7-ethyl-3-(thiophen-2-yl)-6,9-dihydro-5H-pyrazolo(3,4-c)-1,2,4-triazolo(4,3-a)pyridine

References

1. Duplantier AJ, et al. J Med Chem. 2007 Jan 25;50(2):344-9.

2. Giembycz MA. Br J Pharmacol. 2008 Oct;155(3):288-90.

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