Synonym
Tofimilast; CP-325366; CP 325366; CP325366; CP-325,366; CP 325,366; CP325,366.
IUPAC/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
InChi Key
DHCOPPHTVOXDKU-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H21N5S/c1-2-14-13-9-10-22-17(15-8-5-11-24-15)19-20-18(22)16(13)23(21-14)12-6-3-4-7-12/h5,8,11-12H,2-4,6-7,9-10H2,1H3
SMILES Code
CCC1=NN(C2CCCC2)C3=C1CCN4C3=NN=C4C5=CC=CS5
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
Preparing Stock Solutions
The following data is based on the
product
molecular weight
339.46
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 |
1: Jaffari S, Forbes B, Collins E, Barlow DJ, Martin GP, Murnane D. Rapid
characterisation of the inherent dispersibility of respirable powders using dry
dispersion laser diffraction. Int J Pharm. 2013 Apr 15;447(1-2):124-31. doi:
10.1016/j.ijpharm.2013.02.034. PubMed PMID: 23434542; PubMed Central PMCID:
PMC3636537.
2: Tralau-Stewart CJ, Williamson RA, Nials AT, Gascoigne M, Dawson J, Hart GJ,
Angell AD, Solanke YE, Lucas FS, Wiseman J, Ward P, Ranshaw LE, Knowles RG.
GSK256066, an exceptionally high-affinity and selective inhibitor of
phosphodiesterase 4 suitable for administration by inhalation: in vitro, kinetic,
and in vivo characterization. J Pharmacol Exp Ther. 2011 Apr;337(1):145-54. doi:
10.1124/jpet.110.173690. PubMed PMID: 21205923.
3: Giembycz MA. Can the anti-inflammatory potential of PDE4 inhibitors be
realized: guarded optimism or wishful thinking? Br J Pharmacol. 2008
Oct;155(3):288-90. doi: 10.1038/bjp.2008.297. PubMed PMID: 18660832; PubMed
Central PMCID: PMC2567889.
4: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp
Clin Pharmacol. 2007 Sep;29(7):467-509. PubMed PMID: 17982511.
5: Duplantier AJ, Bachert EL, Cheng JB, Cohan VL, Jenkinson TH, Kraus KG,
McKechney MW, Pillar JD, Watson JW. SAR of a series of
5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent
inhibitors of human eosinophil phosphodiesterase. J Med Chem. 2007 Jan
25;50(2):344-9. PubMed PMID: 17228876.
