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Merck
Összes fotó(1)

Fontos dokumentumok

SML0585

Sigma-Aldrich

Piclamilast

≥98% (HPLC)

Szinonimák:

3-(Cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxy-benzamide, N-(3,5-Dichloropyrid-4-yl)-3-cyclopentyloxy-4-methoxybenzamide, RP 73-401, RP 73401, RPR 73401

Bejelentkezésa Szervezeti és Szerződéses árazás megtekintéséhez
Összes fotó(1)

About This Item

Tapasztalati képlet (Hill-képlet):
C18H18Cl2N2O3
CAS-szám:
144035-83-6
Molekulatömeg:
381.25
UNSPSC kód:
41106305
NACRES:
NA.77

Minőségi szint

100

Teszt

≥98% (HPLC)

Forma

powder

szín

white to beige

oldhatóság

DMSO: 20 mg/mL, clear

tárolási hőmérséklet

2-8°C

SMILES string

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)

Nemzetközi kémiai azonosító kulcs

RRRUXBQSQLKHEL-UHFFFAOYSA-N

Alkalmazás

Piclamilasthas been used as a phosphodiesterase-4 (PDE4) inhibitor to treat cultures at the indicated time points after blast exposure.

Biokémiai/fiziológiai hatások

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 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).

Tulajdonságok és előnyök

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.

Piktogramok

Exclamation mark
GHS07

Figyelmeztetés

Warning

Figyelmeztető mondatok

H315,H319,H335

Veszélyességi osztályok

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

Célzott szervek

Respiratory system

Tárolási osztály kódja

11 - Combustible Solids

WGK

WGK 3

Lobbanási pont (F)

Not applicable

Lobbanási pont (C)

Not applicable

Válasszon a legfrissebb verziók közül:

Analitikai tanúsítványok (COA)

Lot/Batch Number
013M4722V

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Dokumentumtár megtekintése

Y P de Visser et al.
The European respiratory journal, 31(3), 633-644 (2007-12-21)
Phosphodiesterase-4 (PDE4) inhibitors may offer novel therapeutic strategies in respiratory diseases, including asthma and chronic obstructive pulmonary disease. Therefore, selective PDE4 inhibitors may also provide a therapeutic option for very pre-term infants with bronchopulmonary dysplasia (BPD). The anti-inflammatory effect of
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
L Wollin et al.
Pulmonary pharmacology & therapeutics, 19(5), 343-352 (2005-11-01)
Roflumilast is an oral, once-daily phosphodiesterase 4 (PDE4) inhibitor with anti-inflammatory activity. We compared the anti-inflammatory effects of roflumilast with those of PDE4 inhibitors rolipram, piclamilast, and cilomilast in ovalbumin (OVA)-sensitized and challenged Brown-Norway rats. Animals were treated orally 1h
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
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
View All Related Papers

Cikkek

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