Aminophylline is a competitive nonselective phosphodiesterase inhibitor that is used to treat airway obstruction from asthma or COPD.
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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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 | ✔ | 98% | |||||||||||||||||
Aminophylline |
+
PDE, IC50: 0.12 mM |
98+% | |||||||||||||||||
Anagrelide HCl | ✔ | 99%+ | |||||||||||||||||
Irsogladine | ✔ | AChR,mAChR | 98% | ||||||||||||||||
PF-8380 |
+++
Autotaxin, IC50: 2.8 nM |
99%+ | |||||||||||||||||
Dipyridamole | ✔ | 98% | |||||||||||||||||
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 | 98% | |||||||||||||||
Pimobendan |
++
PDE3, IC50: 0.32 μM |
98% | |||||||||||||||||
Cilostazol |
++
PDE3, IC50: 0.2 μM |
98% | |||||||||||||||||
Fenspiride HCl |
+
PDE3, pIC50: 3.44 |
+
PDE4, pIC50: 4.16 |
98% | ||||||||||||||||
(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 |
98% | |||||||||||||||||
Vardenafil HCl Trihydrate |
++++
PDE5, IC50: 0.7 nM |
98% | |||||||||||||||||
Tadalafil |
++++
PDE5, IC50: 1.8 nM |
98% | |||||||||||||||||
Icariin |
++
PDE5, IC50: 0.432 μM |
98% | |||||||||||||||||
Sildenafil | ✔ |
+++
PDE6, IC50: 33 nM |
98% | ||||||||||||||||
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 | Intracellular cyclic nucleotide levels can be controlled through regulation of either synthesis via respective cyclases or degradation via the phosphodiesterases (PDEs)[3]. Theophylline, a methylxanthine cyclic adenosine 3'5' monophosphate phosphodiesterase inhibitor, increases intracellular cAMP content and also stimulates fetal lung surfactant synthesis. Aminophylline is the ethylene diamine salt of theophylline[4]. It establishes capabilities to inhibit the cyclic AMP phosphodiesterase and cyclic GMP phosphodiesterase from human lung with I50 values of 0.16 mM and 0.138 mM at 1 μM cyclic AMP and 1 μM cyclic GMP, respectively[3]. Treatment with aminophylline for 24 hours resulted in a 25% (P less than 0.025) decrease in the glycogen content of the explants and glycogen synthase I activity was reduced by 32% in aminophylline treated cultures (P < 0.025)[4]. At higher concentrations (1 and 5 mM), aminophylline significantly elevated the basal cyclic AMP levels of the mouse vas deferens and markedly inhibited the contractile response to various frequencies of stimulation[5]. In five normal and five asthmatic subjects, the plasma cyclic AMP response to isoprenaline aerosol inhalation was enhanced by aminophylline, although to a lesser degree in the asthmatic subjects[6]. |
Dose | Mice: 10 mg/kg[3] (i.p.) |
Administration | i.p. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT03296202 | - | Recruiting | July 2021 | France ... 展开 >> service de médecine interne - CH d'Agen Not yet recruiting Agen, France, 47923 Contact: Patrick RISPAL, MD rispalp@ch-agen.fr Principal Investigator: Patrick RISPAL, MD service de maladies infectieuses - CH de la Côte Basque Recruiting Bayonne, France, 64109 Contact: Marc-Olivier VAREIL, MD movareil@ch-cotebasque.fr Principal Investigator: Marc-Olivier VAREIL, MD service de médecine inter et maladies infectieuses - Hopital Saint André Recruiting Bordeaux, France, 33075 Contact: Patrick MERCIE, Prof patrick.mercie@chu-bordeaux.fr Principal Investigator: Patrick MERCIE, Prof service de médecine interne et maladies infectieuses - Hôpital Saint-André Recruiting Bordeaux, France, 33075 Contact: Fabrice BONNET, Prof fabrice.bonnet@chu-bordeaux.fr Principal Investigator: Fabrice BONNET, Prof service de maladies infectieuses et médecine tropicale - Hôpital Pellegrin Recruiting Bordeaux, France, 33076 Contact: MALVY Denis, Prof denis.malvy@chu-bordeaux.fr Principal Investigator: Denis MALVY, Prof service de maladies infectieuses et médecine tropicale - Hôpital Pellegrin Recruiting Bordeaux, France, 33076 Contact: Didier NEAU, Prof didier.neau@chu-bordeaux.fr Principal Investigator: Didier NEAU, Prof service de maladies infectieuses et médecine tropicale - Hôpital Pellegrin Recruiting Bordeaux, France, 33076 Contact: DUPON Michel, Prof michel.dupon@chu-bordeaux.fr Principal Investigator: DUPON Michel, Prof Service D'Urgences Pédiatriques Recruiting Bordeaux, France Contact: Camille RUNEL-BELLIARD, MD camille.runel@chu-bordeaux.fr Principal Investigator: Camille RUNEL-BELLIARD, MD service de médecine interne et maladies infectieuses - CH de Dax Recruiting Dax, France, 40107 Contact: Yann GERARD, MD gerardy@ch-dax.fr Principal Investigator: Yann GERARD, MD service de médecine interne - CH d'Arcachon Recruiting La Teste-de-Buch, France, 33260 Contact: Carine COURTAULT, MD carine.courtault@ch-arcachon.fr Principal Investigator: Carine COURTAULT, MD service de médecine interne - CH de Libourne Not yet recruiting Libourne, France, 33505 Contact: Helene FERRAND, MD helene.ferrand@ch-libourne.fr Sub-Investigator: Sten DE WITTE, MD Principal Investigator: Helene FERRAND, MD service de médecine interne - CH de Mont de Marsan Not yet recruiting Mont-de-Marsan, France, 40024 Contact: Maud FOISSAC, MD maud.foissac@ch-mt-marsan.fr Principal Investigator: Maud FOISSAC, MD service de médecine interne - CH d'Orthez Recruiting Orthez, France Contact: Yann GERARD, MD gerardy@ch-dax.fr Principal Investigator: Yann GERARD, MD service de médecine interne et maladies infectieuses - CH de Pau Recruiting Pau, France, 64000 Contact: Eric MONLUN, MD eric.monlun@ch-pau.fr Principal Investigator: Eric MONLUN, MD service de médecine interne et maladies infectieuses - CH de Périgueux Recruiting Perigueux, France, 24019 Contact: Philippe LATASTE, MD philippe.lataste@ch-perigueux.fr Principal Investigator: Philippe LATASTE, MD service de médecine interne et maladies infectieuses - Groupe hospitalier Sud Recruiting Pessac, France Contact: Jean-François VIALLARD, Prof jean-francois.viallard@chu-bordeaux.fr Sub-Investigator: Jean-Luc PELLEGRIN, Prof Principal Investigator: Jean-François VIALLARD, Prof service de maladies infecteieuses - CH Saint-Cyr Not yet recruiting Villeneuve sur Lot, France, 47307 Contact: Isabelle CHOSSAT, MD isabelle.chossat@ch-stcyr.fr Principal Investigator: Isabelle CHOSSAT, MD 收起 << | |
NCT02997605 | RheumatoId Arthritis | Phase 4 | Recruiting | December 2019 | France ... 展开 >> Bordeaux University Hospital Recruiting Bordeaux, France Contact: Chirstophe RICHEZ, MD Brest University Hospital Recruiting Brest, France Contact: Alain SARAUX, MD Clermont-Ferrand Hospital Recruiting Clermont-Ferrand, France Contact: Martin SOUBRIER, MDR Bicêtre Hospital Recruiting Le Kremlin-Bicêtre, France Contact: Xavier MARIETTE, MD Lille Hospital Recruiting Lille, France Contact: René-Marc FLIPO, MD Limoges Hospital Recruiting Limoges, France Contact: Pascale Vergne-Salle, MD Montpellier Hospital Recruiting Montpellier, France Contact: Jacques MOREL, MD Orléans Hospital Recruiting Orléans, France Contact: Carine SALLIOT, MD Bichat Hospital Recruiting Paris, France Contact: Philippe DIEUDE, MD Cochin Hospital Recruiting Paris, France Contact: Yannick Allanore, md Principal Investigator: Minh Nguyen, MD La Pitié-Salpétrière Recruiting Paris, France Contact: Laure Gossec, MD Strasbourg Hospital Recruiting Strasbourg, France Contact: Jacques-Eric Gottenberg, MD Hospital Pierre-Paul Riquet Recruiting Toujouse, France, 31059 Contact: Adeline RUYSSEN-WITRAND, MD, PhD 05 61 77 56 26 ext 33 ruyssen-witrand.a@chu-toulouse.fr Contact: Arnaud CONSTANTIN, MD, PhD 05 61 77 69 76 ext 33 constantin.a@chu-toulouse.fr 收起 << |
NCT03421184 | Lupus Erythematosus ... 展开 >> Rheumatoid Arthritis Autoimmune Thrombocytopenia 收起 << | Not Applicable | Recruiting | November 2020 | France ... 展开 >> CHU de Bordeaux - service de médecine interne Recruiting Pessac, France Contact: Jean-François VIALLARD, Prof 05.57.65.64.83 ext +33 jean-françois.viallard@chu-bordeaux.fr Contact: Isabelle RAYMOND, Pharm Principal Investigator: Jean-François VIALLARD, Prof Sub-Investigator: Estibaliz LAZARO, Prof Sub-Investigator: Jean-Luc PELLEGRIN, Prof Sub-Investigator: Carine GREIB, MD Sub-Investigator: Irene MACHELARD, MD Sub-Investigator: Marion MIRABEL, MD Sub-Investigator: Etienne RIVIERE, MD Sub-Investigator: Thierry SCHAEVERBEKE, Prof Sub-Investigator: Christophe RICHEZ, Prof Sub-Investigator: Marie-Elise TRUCHETET, MD Sub-Investigator: Nicolas POURSAC, MD Sub-Investigator: Nadia MEHSEN, MD 收起 << |
[1]Essayan DM. Cyclic nucleotide phosphodiesterases. J Allergy Clin Immunol. 2001 Nov;108(5):671-80.
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.38mL 0.48mL 0.24mL |
11.89mL 2.38mL 1.19mL |
23.79mL 4.76mL 2.38mL |
CAS号 | 317-34-0 |
分子式 | C16H24N10O4 |
分子量 | 420.426 |
别名 | Phyllocontin |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Store in freezer, under -20°C |
溶解度 |
DMSO: 15 mg/mL(35.68 mM),配合低频超声助溶,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 H2O: 6 mg/mL(14.27 mM),配合低频超声助溶 |
动物实验配方 |