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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $44 | In Stock | |
5 mg | $98 | In Stock | |
10 mg | $163 | In Stock | |
25 mg | $328 | In Stock | |
50 mg | $529 | In Stock | |
100 mg | $753 | In Stock | |
1 mL x 10 mM (in DMSO) | $113 | In Stock |
Description | Piclamilast (RP 73401) is a PDE4 inhibitor. |
Targets&IC50 | PDE4:16 nM (pig aorta), PDE2:40 μM, PDE5:14 μM, PDE3:>100 μM, PDE1:>100 μM, 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]. |
Alias | RPR 73401, RP 73401 |
Molecular Weight | 381.25 |
Formula | C18H18Cl2N2O3 |
Cas No. | 144035-83-6 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 30 mg/mL (78.69 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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