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Merck
모든 사진(1)

주요 문서

SML0585

Sigma-Aldrich

Piclamilast

≥98% (HPLC)

동의어(들):

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

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크기 선택

5 MG
₩195,692
25 MG
₩621,789

₩195,692


구입 가능 여부는 고객센터에 문의하십시오.
기존과 동일한 품질을 인하된 가격으로 - 어려운 예산 상황을 머크와 함께 극복하세요


크기 선택

보기 변경
5 MG
₩195,692
25 MG
₩621,789

About This Item

실험식(Hill 표기법):
C18H18Cl2N2O3
CAS Number:
Molecular Weight:
381.25
UNSPSC 코드:
41106305
NACRES:
NA.77

₩195,692


구입 가능 여부는 고객센터에 문의하십시오.
기존과 동일한 품질을 인하된 가격으로 - 어려운 예산 상황을 머크와 함께 극복하세요

분석

≥98% (HPLC)

양식

powder

색상

white to beige

solubility

DMSO: 20 mg/mL, clear

저장 온도

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)

InChI key

RRRUXBQSQLKHEL-UHFFFAOYSA-N

애플리케이션

Piclamilasthas been used as a phosphodiesterase-4 (PDE4) inhibitor to treat cultures at the indicated time points after blast exposure.[1]

생화학적/생리학적 작용

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).[2]

특징 및 장점

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.

픽토그램

Exclamation mark

신호어

Warning

유해 및 위험 성명서

Hazard Classifications

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

표적 기관

Respiratory system

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


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시험 성적서(COA)

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문서 라이브러리 방문

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
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
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

문서

고리형 AMP(cAMP), 고리형 GMP(cGMP), 고리형 ADP-리보스를 포함하여 고리형 뉴클레오타이드는 GPCR 활성화에 의해 개시된 세포내 이벤트의 2차 전달자로서 광범위하게 연구되었습니다. cAMP는 주로 cAMP 의존성 단백질 인산화효소(PKA)의 활성화를 통해 모든 진핵생물 세포에서 세포 기능을 변형시키지만 cAMP 개폐 이온 채널 및 cAMP에 의해 직접 활성화되는 구아닌 뉴클레오타이드 교환 인자를 통해서도 변형시킵니다.

Cyclic nucleotides like cAMP modulate cell function via PKA activation and ion channels.

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