货号:A168666
同义名:
APTA-2217;BYK 20869
Roflumilast is a selective and long-acting inhibitor of PDE-4 with IC50 of 0.8 nM.
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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。 |
靶点 |
|
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]. |
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 |
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 |
|
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 << |
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 |
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 |