Aminophylline 是一种竞争性、非选择性磷酸二酯酶(PDE)抑制剂,亦是一种竞争性腺苷受体拮抗剂;其具备肺血管及支气管扩张活性,可用于哮喘体外或体内机制研究。
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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+ |


| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
|---|---|---|---|---|---|---|---|
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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 |
95% | |||||||||||||||||
| 7-(2,3-Dihydroxypropyl)theophylline | ✔ | 98% | |||||||||||||||||
| Aminophylline |
+
PDE, IC50: 0.12 mM |
98+% | |||||||||||||||||
| Anagrelide HCl | ✔ | 99%+ | |||||||||||||||||
| Irsogladine | ✔ | AChR,mAChR | 99% | ||||||||||||||||
| PF-8380 |
+++
Autotaxin, IC50: 2.8 nM |
99%+ | |||||||||||||||||
| Dipyridamole | ✔ | 98% | |||||||||||||||||
| Balipodect |
++++
PDE10A, IC50: 0.3 nM |
99%+ | |||||||||||||||||
| 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 |
98% | |||||||||||||||||
| Cilostazol |
++
PDE3, IC50: 0.2 μM |
98% | |||||||||||||||||
| Fenspiride HCl |
+
PDE3, pIC50: 3.44 |
+
PDE4, pIC50: 4.16 |
99% (HPLC) | ||||||||||||||||
| (S)-(+)-Rolipram |
++
PDE4, IC50: 0.75 μM |
99% (HPLC) | |||||||||||||||||
| Apremilast |
+++
PDE4, IC50: 74 nM |
98% | |||||||||||||||||
| GSK256066 |
++++
PDE4B, IC50: 3.2 pM |
98+% | |||||||||||||||||
| Roflumilast |
++++
PDE4A1, IC50: 0.7 nM PDE4A4, IC50: 4.3 nM |
99% | |||||||||||||||||
| Rolipram |
+++
PDE4B, IC50: 130 nM |
99%+ | |||||||||||||||||
| Cilomilast |
+++
HPDE4, IC50: 120 nM LPDE4, IC50: 100 nM |
99% | |||||||||||||||||
| 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]. |
| Concentration | Treated Time | Description | References | |
| mouse primordial follicle oocytes | 50 μM | 4 days | promoted mouse primordial follicle activation, increased cAMP levels and p-Akt levels | Int J Biol Sci. 2024 Sep 30;20(13):5312-5329 |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | Naturally aged mouse model | Oral | 4.0 mM | One week administration followed by three weeks observation | Ameliorated infertility in naturally aged mice by improving ovulated oocyte quantity and quality | Int J Biol Sci. 2024 Sep 30;20(13):5312-5329 |
| SD rats | Sepsis model | Intraperitoneal injection | 50 mg/kg | Single dose | To evaluate the effect of aminophylline on gut microbiome and metabolites in septic rats, results showed that aminophylline significantly modulated the gut microbiome and metabolites in septic rats, bringing them closer to the state of healthy rats. | J Transl Med. 2022 Feb 3;20(1):69 |
| Zebrafish | Sapje and sapje-like mutants | Water immersion | 2.5 μg/mL | From 4 dpf to 30 dpf | Aminophylline treatment significantly improved muscle structure and function, increased survival rate, and upregulated the cAMP-dependent PKA pathway activity in dystrophin-deficient zebrafish. | Proc Natl Acad Sci U S A. 2011 Mar 29;108(13):5331-6 |
| 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 | 420.43 |
| SMILES Code | O=C(N1C)N(C)C2=C(NC=N2)C1=O.O=C(N3C)N(C)C4=C(NC=N4)C3=O.NCCN |
| MDL No. | MFCD00013221 |
| 别名 | Phyllocontin |
| 运输 | 蓝冰 |
| InChI Key | FQPFAHBPWDRTLU-UHFFFAOYSA-N |
| Pubchem ID | 9433 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, store in freezer, under -20°C |
| 溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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