Tofimilast ( CP-325366 )

Catalog No. M12872 CAS No. 185954-27-2

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Datasheet

HNMR

HPLC

MSDS

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Product Name

Tofimilast
Note

Research use only, not for human use.
Brief Description

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

Tofimilast (CP-325366) is a potent, selective PDE4 inhibitor with IC50 of 23, 13 and 13 nM for PDE4A, PDE4B, and PDE4D, respectively; shows weakly or no inhibition for PDE4C, and no activity for PDE1, PDE2, PDE3, PDE5, PDE6, and PDE7; 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; shows low oral bioavailability and no emesis-associated behaviors in the ferret emesis model.Asthma Discontinued
Synonyms

CP-325366
Pathway

Angiogenesis
Target

PDE
Recptor

PDE
Research Area

Inflammation/Immunology
Indication

Asthma

CAS Number

185954-27-2
Formula Weight

339.46
Molecular Formula

C18H21N5S
Purity

>98% (HPLC)
Solubility

——
SMILES

CCC1=NN(C2CCCC2)C3=C1CCN4C3=NN=C4C5=CC=CS5
Chemical Name

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

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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