西洛司特

更新时间：2025-08-25 13:32:29

西洛司特结构式	常用名	西洛司特	英文名	Cilomilast
	CAS号	153259-65-5	分子量	343.417
	密度	1.2±0.1 g/cm3	沸点	549.1±50.0 °C at 760 mmHg
	分子式	C₂₀H₂₅NO₄	熔点	157ºC
	MSDS	中文版美版	闪点	285.9±30.1 °C

西洛司特用途

Cilomilast(SB 207499; Ariflo)是PDE4抑制剂,IC50为110 nM,有抗炎活性。

中文名	西洛司特
英文名	4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)cyclohexane-1-carboxylic acid
中文别名	替吡法尼 \| 4-氰基-4-(3-环戊氧基-4-甲氧基苯基)环己烷-1-甲酸
英文别名	更多

描述	Cilomilast(SB 207499; Ariflo)是PDE4抑制剂,IC50为110 nM,有抗炎活性。
相关类别	信号通路 >> 代谢酶/蛋白酶 >> 磷酸二酯酶(PDE) 研究领域 >> 炎症/免疫
参考文献	[1]. MARY S. BARNETTE et al. SB 207499 (Ariflo), a Potent and Selective Second-Generation Phosphodiesterase 4 Inhibitor: In Vitro Anti-inflammatory Actions JPET 284:420 -426, 1998 [2]. Munisso MC, Kang JH, Tsurufuji M, Yamaoka T.Cilomilast enhances osteoblast differentiation of mesenchymal stem cells and bone formation induced by bone morphogenetic protein 2.Biochimie. 2012 Jun 15. [3]. Sadrai Z, Stevenson W, Okanobo A, Chen Y, Dohlman TH, Hua J, Amparo F, Chauhan SK, Dana R.PDE4 inhibition suppresses IL-17-associated immunity in dry eye disease.Invest Ophthalmol Vis Sci. 2012 Jun 14;53(7):3584-91. Print 2012 Jun. [4]. Pace E, Ferraro M, Uasuf CG, Giarratano A, La Grutta S, Liotta G, Johnson M, Gjomarkaj M.Cilomilast counteracts the effects of cigarette smoke in airway epithelial cells.Cell Immunol. 2011;268(1):47-53. Epub 2011 Feb 20. [5]. Barton AK, Niedorf F, Gruber AD, Kietzmann M, Ohnesorge B.Pharmacological studies of bronchial constriction inhibited by parasympatholytics and cilomilast using equine precision-cut lung slices.Berl Munch Tierarztl Wochenschr. 2010 May-Jun;123(5-6):229-35

描述

Cilomilast(SB 207499; Ariflo)是PDE4抑制剂,IC50为110 nM,有抗炎活性。

相关类别

信号通路 >> 代谢酶/蛋白酶 >> 磷酸二酯酶(PDE)

研究领域 >> 炎症/免疫

参考文献

[1]. MARY S. BARNETTE et al. SB 207499 (Ariflo), a Potent and Selective Second-Generation Phosphodiesterase 4 Inhibitor: In Vitro Anti-inflammatory Actions JPET 284:420 -426, 1998

[2]. Munisso MC, Kang JH, Tsurufuji M, Yamaoka T.Cilomilast enhances osteoblast differentiation of mesenchymal stem cells and bone formation induced by bone morphogenetic protein 2.Biochimie. 2012 Jun 15.

[3]. Sadrai Z, Stevenson W, Okanobo A, Chen Y, Dohlman TH, Hua J, Amparo F, Chauhan SK, Dana R.PDE4 inhibition suppresses IL-17-associated immunity in dry eye disease.Invest Ophthalmol Vis Sci. 2012 Jun 14;53(7):3584-91. Print 2012 Jun.

[4]. Pace E, Ferraro M, Uasuf CG, Giarratano A, La Grutta S, Liotta G, Johnson M, Gjomarkaj M.Cilomilast counteracts the effects of cigarette smoke in airway epithelial cells.Cell Immunol. 2011;268(1):47-53. Epub 2011 Feb 20.

[5]. Barton AK, Niedorf F, Gruber AD, Kietzmann M, Ohnesorge B.Pharmacological studies of bronchial constriction inhibited by parasympatholytics and cilomilast using equine precision-cut lung slices.Berl Munch Tierarztl Wochenschr. 2010 May-Jun;123(5-6):229-35

密度	1.2±0.1 g/cm3
沸点	549.1±50.0 °C at 760 mmHg
熔点	157ºC
分子式	C₂₀H₂₅NO₄
分子量	343.417
闪点	285.9±30.1 °C
精确质量	343.178345
PSA	79.55000
LogP	3.30
InChIKey	CFBUZOUXXHZCFB-UHFFFAOYSA-N
SMILES	COc1ccc(C2(C#N)CCC(C(=O)O)CC2)cc1OC1CCCC1
外观性状	白色固体
蒸汽压	0.0±1.6 mmHg at 25°C
折射率	1.568
储存条件	?20°C
水溶解性	DMSO: soluble15mg/mL, clear

西洛司特MSDS英文版

危险品运输编码	NONH for all modes of transport

methyl 4-cyano-...

153259-59-7

~54%

西洛司特

153259-65-5

文献：SmithKline Beecham Corporation Patent: US5602157 A1, 1997 ;

methyl trans-[4...

153259-61-1

~45%

西洛司特

153259-65-5

文献：Christensen, Siegfried B.; Guider, Aimee; Forster, Cornelia J.; Gleason, John G.; Bender, Paul E.; Karpinski, Joseph M.; Dewolf Jr., Walter E.; Barnette, Mary S.; Underwood, David C.; Griswold, Don E.; Cieslinski, Lenora B.; Burman, Miriam; Bochnowicz, Steven; Osborn, Ruth R.; Manning, Carol D.; Grous, Marilyn; Hillegas, Leonard M.; Bartus, Joan O'Leary; Dominic Ryan; Eggleston, Drake S.; Curtis Haltiwanger; Torphy, Theodore J. Journal of Medicinal Chemistry, 1998 , vol. 41, # 6 p. 821 - 835

1-[3-(CYCLOPENT...

152630-47-2

西洛司特

153259-65-5

文献：Journal of Organic Chemistry, , vol. 67, # 15 p. 5440 - 5443

2-[4-cyano-4-(3...

153260-05-0

西洛司特

153259-65-5

文献：Journal of Medicinal Chemistry, , vol. 41, # 6 p. 821 - 835

西洛司特上游产品 1
CAS号152630-47-2 1-[3-(CYCLOPENT...
西洛司特下游产品 0

Blockade of PDE4B limits lung vascular permeability and lung inflammation in LPS-induced acute lung injury.

Biochem. Biophys. Res. Commun. 450(4) , 1560-7, (2014)

Acute lung injury (ALI), acute respiratory distress syndrome (ARDS), is actually involved in an ongoing and uncontrolled inflammatory response in lung tissues. Although extensive studies suggested tha...

cis-4-(3-(Cyclopentyloxy)-4-methoxyphenyl)-4-cyanocyclohexane-1-carboxylic acid

1xlx

cis-4-Cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)cyclohexanecarboxylic acid

cis-4-Cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexanecarboxylic acid

S1455_Selleck

Ariflo

c-4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)-r-1-cyclohexane carboxylic acid

1xom

cilomilast

4-Cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexanecarboxylic acid

SB-207499