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磷酸二酯酶抑制剂
/ Roflumilast

罗氟司特 /Roflumilast 99%

货号：A168666 同义名： APTA-2217;BYK 20869 Ambeed 开学季，买赠积分，赢豪礼

Roflumilast is a selective and long-acting inhibitor of PDE-4 with IC50 of 0.8 nM.

Roflumilast 化学结构 CAS号：162401-32-3
Roflumilast 化学结构
CAS号：162401-32-3
Roflumilast 3D分子结构
CAS号：162401-32-3
Roflumilast 化学结构 CAS号：162401-32-3
Roflumilast 3D分子结构 CAS号：162401-32-3
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Roflumilast 纯度/质量文件 产品仅供科研

货号：A168666 标准纯度： 99%
批次查询： 批次纯度:

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产品名称 PDE ↓ PDE1 ↓ PDE10A ↓ PDE2 ↓ PDE3 ↓ PDE4 ↓ PDE5 ↓ PDE6 ↓ 其他靶点 纯度
Doxofylline ✔ 99+%
Deltarasin +++

PDEδ , Kd: 38 nM

 		99+%
7-(2,3-Dihydroxypropyl)theophylline ✔ 99%+
Aminophylline +

PDE, IC50: 0.12 mM

 		99%+
Anagrelide HCl ✔ 99%+
Irsogladine ✔ mAChR,AChR 99%+
PF-8380 +++

Autotaxin, IC50: 2.8 nM

 		99%+
Dipyridamole ✔ 99%+
Balipodect ++++

PDE10A, IC50: 0.3 nM

 		99%+
PF-2545920 ++++

PDE10A, IC50: 0.37 nM

 		97%
Luteolin +

PDE1, Ki: 15.0 μM

 		++

PDE2, Ki: 6.4 μM

 		+

PDE3, Ki: 13.9 μM

 		+

PDE4, Ki: 11.1 μM

 		+

PDE5, Ki: 9.5 μM

 		98%
Milrinone ++

PDE2, IC50: 5.2 μM

 		++

PDE3, IC50: 2.1 μM

 		ATPase 99%+
Pimobendan ++

PDE3, IC50: 0.32 μM

 		99%+
Cilostazol ++

PDE3, IC50: 0.2 μM

 		99%+
Fenspiride HCl +

PDE3, pIC50: 3.44

 		+

PDE4, pIC50: 4.16

 		99%+
(S)-(+)-Rolipram ++

PDE4, IC50: 0.75 μM

 		98%
Apremilast +++

PDE4, IC50: 74 nM

 		98%
GSK256066 ++++

PDE4B, IC50: 3.2 pM

 		98+%
Roflumilast ++++

PDE4A4, IC50: 4.3 nM

PDE4A1, IC50: 0.7 nM

 		99%
Rolipram +++

PDE4B, IC50: 130 nM

 		99%+
Cilomilast +++

LPDE4, IC50: 100 nM

HPDE4, IC50: 120 nM

 		98+%
Avanafil ++++

PDE5, IC50: 1 nM

 		99%+
Vardenafil HCl Trihydrate ++++

PDE5, IC50: 0.7 nM

 		99%+
Tadalafil ++++

PDE5, IC50: 1.8 nM

 		98%
Icariin ++

PDE5, IC50: 0.432 μM

 		98%
Sildenafil ✔ +++

PDE6, IC50: 33 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Roflumilast 生物活性

靶点

  • PDE4

    PDE4A4, IC50:4.3 nM

    PDE4A1, IC50:0.7 nM
描述 Phosphodiesterases (PDEs) are a family of enzymes that catalyze the hydrolysis of cyclic adenosine monophosphate and cyclic guanosine monophosphate. Roflumilast is a potent inhibitor of both human PDE4B and PDE4D with IC50 values of 0.84 and 0.68nM, respectively, while it showed much less inhibitory activity against other forms of PDEs (IC50 values > 10μM)[7]. In A549 cells, roflumilast at the dose of 1μM prevented EGF-stimulated increase in MUC5AC mRNA and protein production but did not change the basal MUC5AC expression, and also inhibited EGF-induced phosphorylation of tyrosine residues of different intracellular proteins (i.e. EGF receptor, phospho-p38- and p44/42-MAPK) and the upregulation of EGFR expression. In human isolated bronchus, the presence of 1μM roflumilast inhibited EGF-induced MUC5AC mRNA and protein expression[8]. In A/J mice expressing wild type cystic fibrosis transmembrane conductance regulator (CFTR) and exposed to cigarette smoke or air, acute roflumilast (30nM) treatment increased CFTR-dependent chloride transport in both smoke- and air-exposed mice as compared to vehicle-treated group. Oral administration of roflumilast (5mg/kg/day, once per day) for five weeks activated CFTR and completely reversed cigarette smoke-induced adverse effects in vivo[9].
作用机制 The difluromethoxy group of roflumilast binds at the Q1 pocket of enzyme, while the cyclopropyl methoxy group binds at the Q2 pocket[7].

Roflumilast 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
HEK293 cells Function assay 15 min Inhibition of PDE4 expressed in HEK293 cells coexpressing cyclic nucleotide gated ion channel mutant assessed as inhibition of NECA-induced cAMP production treated 15 mins before NECA challenge measured after 45 mins by FLIPR assay 20378348
PBMC Function assay Inhibition of TNFalpha production in LPS-stimulated human PBMC preincubated before LPS challenge measured after 4 hrs by enzyme immunoassay, IC50=2e-05 μM 19256507
sf21 cells Function assay Inhibition of human full length PDE4A4 expressed in baculovirus infected sf21 cells, IC50=0.35 nM 23806553

Roflumilast 动物研究

Dose Guinea pig: 0.04 mg/kg - 4 mg/kg[3] (p.o.) Mice: 1 mg/kg, 5 mg/kg[4] (p.o.), 5 mg/kg - 10 mg/kg[5] (p.o.)
Administration p.o.
Pharmacokinetics
Animal Mice[6] Rats[6] Dogs[6] Monkeys[6]
Dose 12 mg/kg 20 mg/kg 2 mg/kg 0.5 mg/kg
Administration p.o. p.o. p.o. p.o.
F 0.25 0.11 0.19 0.48
Vd 1.9 L/kg 5.1 L/kg 2.1 L/kg 2.1 L/kg
T1/2 0.7 h 0.9 h 3.8 h 4.4 h
CL 1.8 L/h/kg 3.9 L/h/kg 0.4 L/h/kg 0.3 L/h/kg
Cmax 1313 μg/ml 94 μg/ml 106 μg/ml 341 μg/ml
AUC0→∞ 1663 μg·h/ml 643 μg·h/ml 1054 μg·h/ml 648 μg·h/ml

Roflumilast 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03762330 Chronic Obstructive Pulmonary ... 展开 >>Disease 收起 << Not Applicable Not yet recruiting January 2021 -
NCT02835716 - Recruiting September 2020 United States, Connecticut ... 展开 >> Millennium Magnetic Technologies, LLC Recruiting Westport, Connecticut, United States, 06880 Contact: Steve Levy, MD    203-423-9494    SL@MilMag.net    Contact: Donald H Marks, MD PhD    9733070364    DHM@MilMag.net 收起 <<
NCT01730404 COPD Phase 2 Completed - Ireland ... 展开 >> Celerion Belfast, Ireland United Kingdom Parexel, early phases Harrow, United Kingdom Medicines Evaluation Unit Ltd Manchester, United Kingdom Freeman Hospital Newcastle, United Kingdom Nottingham University Hospitals NHS Trust Nottingham, United Kingdom 收起 <<

Roflumilast 参考文献

[1]Martorana PA, Lunghi B, et al. Effect of roflumilast on inflammatory cells in the lungs of cigarette smoke-exposed mice. BMC Pulm Med. 2008 Aug 28;8:17.

[2]Hatzelmann A, Schudt C. Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J Pharmacol Exp Ther. 2001 Apr;297(1):267-79.

[3]Wollin L, Marx D, et al. Roflumilast inhibition of pulmonary leukotriene production and bronchoconstriction in ovalbumin-sensitized and -challenged Guinea pigs. J Asthma. 2005 Dec;42(10):873-8.

[4]Martorana PA, Beume R, et al. Roflumilast fully prevents emphysema in mice chronically exposed to cigarette smoke. Am J Respir Crit Care Med. 2005 Oct 1;172(7):848-53. Epub 2005 Jun 16.

[5]Kasetty G, Papareddy P, et al. Roflumilast Increases Bacterial Load and Dissemination in a Model of Pseudomononas Aeruginosa Airway Infection. J Pharmacol Exp Ther. 2016 Apr;357(1):66-72.

[6]Roflumilast

[7]Card GL, England BP, Suzuki Y, Fong D, Powell B, Lee B, Luu C, Tabrizizad M, Gillette S, Ibrahim PN, Artis DR, Bollag G, Milburn MV, Kim SH, Schlessinger J, Zhang KY. Structural basis for the activity of drugs that inhibit phosphodiesterases. Structure. 2004 Dec;12(12):2233-47.

[8]Mata M, Sarriá B, Buenestado A, Cortijo J, Cerdá M, Morcillo EJ. Phosphodiesterase 4 inhibition decreases MUC5AC expression induced by epidermal growth factor in human airway epithelial cells. Thorax. 2005 Feb;60(2):144-52.

[9]Raju SV, Rasmussen L, Sloane PA, Tang LP, Libby EF, Rowe SM. Roflumilast reverses CFTR-mediated ion transport dysfunction in cigarette smoke-exposed mice. Respir Res. 2017 Sep 18;18(1):173.

Roflumilast 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.48mL

0.50mL

0.25mL

12.40mL

2.48mL

1.24mL

24.80mL

4.96mL

2.48mL

Roflumilast 技术信息

CAS号162401-32-3
分子式C17H14Cl2F2N2O3
分子量 403.21
别名 APTA-2217;BYK 20869;Daliresp;Daxas;BY 217;B9302-107
运输蓝冰
存储条件

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 50 mg/mL(124 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Roflumilast | APTA-2217;BYK 20869;Daliresp;Daxas;BY 217;B9302-107 | Phosphodiesterase Inhibitor | PDE | AmBeed-信号通路专用抑制剂 | Roflumilast 纯度/质量文件 | Roflumilast 亚型比较 | Roflumilast 生物活性 | Roflumilast 细胞研究 | Roflumilast 动物研究 | Roflumilast 临床数据 | Roflumilast 参考文献 | Roflumilast 实验方案 | Roflumilast 技术信息

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