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Submit ReviewPiclamilast is a potent and selective inhibitor of phosphodiesterase (PDE) 4 (IC50 = 1 nM at PDE4 from human neutrophils). Displays >19,000-fold selectivity over other PDE isoenzymes. Exhibits anti-inflammatory effects in models of allergic inflammation. Also inhibits LTB4 synthesis in human neutrophils (IC50 = 2 nM).
Piclamilast is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 381.25 |
公式 | C18H18Cl2N2O3 |
储存 | Store at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 144035-83-6 |
PubChem ID | 154575 |
InChI Key | RRRUXBQSQLKHEL-UHFFFAOYSA-N |
Smiles | O=C(NC3=C(Cl)C=NC=C3Cl)C1=CC(OC2CCCC2)=C(OC)C=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 38.12 | 100 |
以下数据基于产品分子量 381.25。 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.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.62 mL | 13.11 mL | 26.23 mL |
5 mM | 0.52 mL | 2.62 mL | 5.25 mL |
10 mM | 0.26 mL | 1.31 mL | 2.62 mL |
50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
参考文献是支持产品生物活性的出版物。
Raeburn et al (1994) Anti-inflammatory and bronchodilator properties of RP 73401, a novel and selective phosphodiesterase type IV inhibitor. Br.J.Pharmacol. 113 1423 PMID: 7889300
Hatzelmann and Schudt (2001) Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflum. in vitro. J.Pharmacol.Exp.Ther. 297 267 PMID: 11259554
Zhao et al (2003) Inhibitor binding to type 4 phosphodiesterase (PDE4) assessed using [3H]piclamilast and [3H]rolipram. J.Pharmacol.Exp.Ther. 305 565 PMID: 12704225
If you know of a relevant reference for Piclamilast, please let us know.
关键词: Piclamilast, Piclamilast supplier, RP73401, phosphodiesterases, pde4, potent, selective, inhibitors, inhibits, RP, 73401, Phosphodiesterases, 4525, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Piclamilast 的部分引用包括:
Zhang et al (2019) PDE1 inhibition facilitates proteasomal degradation of misfolded proteins and protects against cardiac proteinopathy. Sci Adv 5 eaaw5870 PMID: 31131329
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