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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 20 mg/mL, clear
储存温度
2-8°C
SMILES字符串
Clc1cncc(c1NC(=O)c2cc(c(cc2)OC)OC3CCCC3)Cl
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)
InChI key
RRRUXBQSQLKHEL-UHFFFAOYSA-N
应用
Piclamilasthas been used as a phosphodiesterase-4 (PDE4) inhibitor to treat cultures at the indicated time points after blast exposure.
生化/生理作用
Piclamilast is a potent and selective cyclic AMP phosphodiesterase-4 inhibitor that exhibits equal, high affinity for both the PDE4 high- and low-affinity rolipram binding states (HARBS and LARBS). Recent studies shown that piclamilast inhibits Trypanosoma brucei PDEB1 (TbrPDEB1) and TbrPDEB2.
Piclamilast is a potent and selective cyclic AMP phosphodiesterase-4 inhibitor.
Piclamilast is also known as N-(3,5-dichloropyrid-4-yl)-3-cyclopentyloxy-4-methoxybenzamide. Piclamilast regulates the cAMP (cyclic adenosine monophosphate) signaling pathway. It increases the retinoid-dependent transactivation and the degradation of retinoic acid receptor α (RARα).
特点和优势
This compound is a featured product for Cyclic Nucleotide research. Click here to discover more featured Cyclic Nucleotide products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the Phosphodiesterases page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
警示用语：
Warning
危险声明
危险分类
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
靶器官
Respiratory system
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
C Méhats et al.
The Journal of clinical endocrinology and metabolism, 86(11), 5358-5365 (2001-11-10)
Elevation of cAMP content resulting from stimulation of the receptor-adenylyl cyclase complex is involved in maintaining the quiescence of the human myometrium during pregnancy. The magnitude of this elevation is critically influenced by the rate of cAMP hydrolysis by phosphodiesterase
Kerryn McCluskie et al.
The Journal of pharmacology and experimental therapeutics, 319(1), 468-476 (2006-07-25)
Phosphodiesterase type 4 (PDE(4)) inhibitors are currently being evaluated as potential therapies for inflammatory airway diseases. However, this class of compounds has been shown to cause an arteritis/vasculitis of unknown etiology in rats and cynomolgus monkeys. Studies in rodents have
Yu Zhao et al.
The Journal of pharmacology and experimental therapeutics, 305(2), 565-572 (2003-04-22)
Piclamilast is a type 4 phosphodiesterase (PDE4) inhibitor with equal affinity for the high-affinity rolipram binding site (HARBS) and low-affinity rolipram binding site (LARBS). The binding of [(3)H]piclamilast to preparations of rat brain and peripheral tissue was investigated and compared
Phosphodiesterase-4 inhibition restored hippocampal long term potentiation after primary blast
Vogel EW, et al.
Experimental Neurology, 293(40), 91-100 (2017)
Sean D McKenna et al.
Endocrinology, 146(1), 208-214 (2004-09-28)
Phosphodiesterases (PDEs) are a family of enzymes that hydrolyze cyclic nucleotides to render them biologically inactive. As such, these enzymes are critical regulators of signal transduction pathways that use cyclic nucleotides as second messengers. PDE4 is one such member that
商品
Cyclic nucleotides like cAMP modulate cell function via PKA activation and ion channels.
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