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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Piclamilast is a novel potent, and selective PDE4 inhibitor. Phosphodiesterase type 4 (PDE4) inhibitors have anti-inflammatory and antioxidant effects, as described in in vivo and in vitro COPD models. This is the first study to demonstrate antioxidant effects of a selective PDE4 inhibitor at the global gene expression level, and the results support the importance of AP-1 as a key regulator of the expression of genes involved in the inflammatory response of epithelial cells to oxidative damage.
ln Vitro |
Piclamilast (RP 73401, 1 μM, 30 minutes) phosphorylates c-Jun Ser63 and activates AP-1 to dramatically block alterations in 23 genes [2]. For RT-PCR of PDE1, PDE2, PDE3, and PDE5[2], use Piclamilast (RP 73401).
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ln Vivo |
In albino animals, piclamilast (RP 73401, 10 mg/kg, 30 minutes) does not alter the MST written on its own. In albino animals, piclamilast plus ATRA increased MST (40 days; interval 34-45 days) more effectively than ATRA alone [3].
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Cell Assay |
RT-PCR[2]
Cell Types: Human A549 type II lung epithelial cells. The IC50 values are >100 μM, 40 μM, >100 μM, and 14 μM respectively [4]. Tested Concentrations: 1 μM (H2O2 200 μM). Incubation Duration: 30 minutes. Experimental Results: Prevented H2O2-induced changes in gene expression levels in A549 cells. Cell viability assay [3] Cell Types: NB4 cells. Tested Concentrations: 30μM. Incubation Duration: 3 days. Experimental Results: Significant enhancement of STAT1 induction observed in ATRA-treated NB4 cells. Resulting in a significant increase in the number of cells expressing NBT-R activity. |
Animal Protocol |
Animal/Disease Models: SCID (severe combined immunodeficient) mouse [3].
Doses: 10 mg/kg (combined with ATRA). Doses: Daily injection. Experimental Results: More effective than ATRA alone in increasing MST (40 days; interval 34-45 days) in animals with leukemia. |
References |
[1]. M J Ashton, et al. Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues. J Med Chem. 1994 May 27;37(11):1696-703.
[2]. Manuel Mata, et al. Piclamilast inhibits the pro-apoptotic and anti-proliferative responses of A549 cells exposed to H(2)O(2) via mechanisms involving AP-1 activation. Free Radic Res. 2012 May;46(5):690-9. [3]. Edoardo Parrella, et al. Phosphodiesterase IV inhibition by piclamilast potentiates the cytodifferentiating action of retinoids in myeloid leukemia cells. Cross-talk between the cAMP and the retinoic acid signaling pathways. J Biol Chem . 2004 Oct 1;279(40):42026-40. [4]. T Ukita, et al. Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives. J Med Chem. 1999 Mar 25;42(6):1088-99. |
Molecular Formula |
C18H18N2O3CL2
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Molecular Weight |
381.25312
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CAS # |
144035-83-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(NC1=C(Cl)C=NC=C1Cl)C2=CC=C(OC)C(OC3CCCC3)=C2
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InChi Key |
RRRUXBQSQLKHEL-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C18H18Cl2N2O3/c1-24-15-7-6-11(8-16(15)25-12-4-2-3-5-12)18(23)22-17-13(19)9-21-10-14(17)20/h6-10,12H,2-5H2,1H3,(H,21,22,23)
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Chemical Name |
3-(Cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-methoxybenzamide
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Synonyms |
Piclamilast; RP-73401; RP 73-401; RP 73401; RP 73 401; RP73401; RP 73401;
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~50 mg/mL (~131.15 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6230 mL | 13.1148 mL | 26.2295 mL | |
5 mM | 0.5246 mL | 2.6230 mL | 5.2459 mL | |
10 mM | 0.2623 mL | 1.3115 mL | 2.6230 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.