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Piclamilast (RP 73401) is a PDE4 inhibitor.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $44 | In Stock | In Stock | |
| 5 mg | $98 | In Stock | In Stock | |
| 10 mg | $163 | In Stock | In Stock | |
| 25 mg | $328 | In Stock | In Stock | |
| 50 mg | $529 | In Stock | In Stock | |
| 100 mg | $753 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $113 | In Stock | In Stock |
| Description | Piclamilast (RP 73401) is a PDE4 inhibitor. |
| Targets&IC50 | PDE2:40 μM, PDE3:>100 μM, PDE1:>100 μM, PDE5:14 μM, PDE4:16 nM (pig aorta), PDE4:2 nM (eosinophil soluble) |
| In vitro | Piclamilast pre-treatment significantly inhibited the changes in 23 genes via mechanisms involving AP-1 activation and c-Jun phosphorylation at Ser63[1]. The IC50s for Piclamilast was 16 nM and 2 nM in pig aorta and eosinophil soluble, respectively. Piclamilast exhibited IC50 values >100 μM, 40 μM, >100 μM, 14 μM for PDE1, PDE2, PDE3 and PDE5. Respectively[4]. |
| In vivo | Initial in vivo studies conducted in severe combined immunodeficiency mice transplanted with NB4 leukemia cells indicate that the enhancing effect of piclamilast on ATRA-induced myeloid maturation translates into a therapeutic benefit[2]. |
| Synonyms | RPR 73401, RP 73401 |
| Molecular Weight | 381.25 |
| Formula | C18H18Cl2N2O3 |
| Cas No. | 144035-83-6 |
| Smiles | COc1ccc(cc1OC1CCCC1)C(=O)Nc1c(Cl)cncc1Cl |
| Relative Density. | 1.37g/cm3 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 30 mg/mL (78.69 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Corn Oil: 2 mg/mL (5.25 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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