Filaminast - CAS 141184-34-1
Catalog number: 141184-34-1
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C15H20N2O4
Molecular Weight:
292.33
COA:
Inquire
Targets:
Phosphodiesterase (PDE)
Description:
Filaminast is a Type 4 cyclic nucleotide phosphodiesterase inhibitor. It is an analog of rolipram which served as a prototype molecule for several development efforts. In Oct 1999, phase II clinical trials for Asthma in European Union was discontinued.
Purity:
98%
Appearance:
Powder
Synonyms:
UNII-CDD69JC61J; Way-pda-641; WAY-PDA 641; WAY-PDA-641; CDD69JC61J; SCHEMBL73843; 1-(3-(Cyclopentyloxy)-4-methoxyphenyl)ethanone-(E)-O-(aminocarbonyl)oxime
Solubility:
Soluble in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Asthma
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
STTRYQAGHGJXJJ-LICLKQGHSA-N
InChI:
1S/C15H20N2O4/c1-10(17-21-15(16)18)11-7-8-13(19-2)14(9-11)20-12-5-3-4-6-12/h7-9,12H,3-6H2,1-2H3,(H2,16,18)/b17-10+
Canonical SMILES:
C(\C)(=N/OC(=O)N)c1cc(c(cc1)OC)OC1CCCC1
Current Developer:
Originator Wyeth
1.Can the anti-inflammatory potential of PDE4 inhibitors be realized: guarded optimism or wishful thinking?
Giembycz MA Br J Pharmacol. 2008 Oct;155(3):288-90. doi: 10.1038/bjp.2008.297. Epub 2008 Jul 28.
PDE4 inhibitors have been in development as a novel anti-inflammatory therapy since the 1980s with asthma and chronic obstructive pulmonary disease (COPD) being primary indications. Despite initial optimism, none have yet reached the market. In most cases, the development of PDE4 inhibitors of various structural classes, including cilomilast, filaminast, lirimilast, piclamilast, tofimilast, AWD-12-281 (aka GSK 842470), CDP840, CI-1018, D-4418, IC485, L-826,141, SCH 351391 and V11294A has been discontinued due to lack of efficacy. A primary problem is the low therapeutic ratio of these compounds, which severely limits the dose that can be given. Indeed, for many of these compounds it is likely that the maximum tolerated dose is either sub-therapeutic or at the very bottom of the efficacy dose-response curve. Therefore, the challenge is to overcome this limitation. It is, therefore, encouraging that many 'new(er)' PDE4 inhibitors in development are reported to have an improved therapeutic window including tetomilast, oglemilast, apremilast, ONO 6126, IPL-512602 and IPL-455903 (aka HT-0712), although the basis for their superior tolerability has not been disclosed. In addition, other approaches are possible that may allow the anti-inflammatory activity of PDE inhibitors to be realized.
2.Phosphodiesterase-IV inhibition, respiratory muscle relaxation and bronchodilation by WAY-PDA-641.
Heaslip RJ;Lombardo LJ;Golankiewicz JM;Ilsemann BA;Evans DY;Sickels BD;Mudrick JK;Bagli J;Weichman BM J Pharmacol Exp Ther. 1994 Feb;268(2):888-96.
The ability of 1-[3-(cyclopentyloxy)-4-methoxyphenyl]ethanone (E)-O-(aminocarbonyl) oxime) (WAY-PDA-641) to inhibit cyclic AMP-metabolizing phosphodiesterases (PDEs) and to relax respiratory muscle was explored as part of a program to identify a PDE-IV inhibitor for potential use in the treatment of asthma. WAY-PDA-641 was identified as a preferential inhibitor of PDE-IV, possessing 36 times greater potency versus canine trachealis PDE-IV than PDE-III (IC50, 4.2 x 10(-7) M and 1.5 x 10(-5) M, respectively). The classification of WAY-PDA-641 as a preferential PDE-IV inhibitor was supported in radioligand binding studies, which demonstrated that 10 microM WAY-PDA-641 did not displace ligands from a large number of receptors, and in functional studies, which used isolated guinea pig tracheal rings. Under conditions in which tracheal rings were made sensitive to the relaxant effects of PDE-IV or PDE-III inhibitors, WAY-PDA-641 induced relaxation with IC50S of 2.6 x 10(-8) M (PDE-IV) and 3.2 x 10(-5) M (PDE-III). Moreover, PDE-IV inhibitory concentrations of WAY-PDA-641 significantly potentiated the relaxant effects of albuterol. WAY-PDA-641 reversed tracheal contractions induced by prostaglandin F2 alpha, leukotriene D4 or histamine in a biphasic manner consistent with its activity as a preferential PDE-IV inhibitor.
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Chemical Structure

CAS 141184-34-1 Filaminast

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