CAS NO: | 292135-78-5 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Roflumilast N-oxide is aPDE type 4inhibitor. | ||||||||||||||||
IC50& Target | PDE type 4[1] | ||||||||||||||||
体外研究 (In Vitro) | Roflumilast N-oxide at 2 nM partly mitigates the cigarette smoke extract (CSE)-induced epithelial to mesenchymal transition (EMT) in WD-HBECin vitro. Roflumilast N-oxide (2 nM) reverses the compromised expression of E-cadherin transcripts following CSE by 45%. The expression of collagen type I is abrogated by Roflumilast N-oxide (2 nM). The epithelial cell phenotype appears protected when cells are co-incubated with Roflumilast N-oxide (2 nM). Pre-incubation with Roflumilast N-oxide (2 nM) also partly attenuates the nuclear translocation of β-catenin[2]. | ||||||||||||||||
体内研究 (In Vivo) | Single treatment ofdb/dbmice with 10 mg/kg Roflumilast N-oxide enhances plasma glucagon-like peptide-1 (GLP-1) 4-fold. Chronic treatment ofdb/dbmice with Roflumilast N-oxide at 3 mg/kg shows prevention of disease progression. Roflumilast-N-oxide abolishes the increase in blood glucose, reduces the increment in HbA1cby 50% and doubles fasted serum insulin compare with vehicle, concomitants with preservation of pancreatic islet morphology. Furthermore, Roflumilast-N-oxide amplifies forskolin-induced insulin release in primary islets. Roflumilast-N-oxide also shows stronger glucose-lowering effects than its parent compound[3]. | ||||||||||||||||
分子量 | 419.21 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C17H14Cl2F2N2O4 | ||||||||||||||||
CAS 号 | 292135-78-5 | ||||||||||||||||
中文名称 | 罗氟司特N-氧化物 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 250 mg/mL(596.36 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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