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Aminophylline/氨茶碱 {[allProObj[0].p_purity_real_show]}

货号:A594330 同义名: Phyllocontin

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
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Aminophylline/氨茶碱 化学结构 CAS号:317-34-0
Aminophylline/氨茶碱 化学结构
CAS号:317-34-0
Aminophylline/氨茶碱 3D分子结构
CAS号:317-34-0
Aminophylline/氨茶碱 化学结构 CAS号:317-34-0
Aminophylline/氨茶碱 3D分子结构 CAS号:317-34-0
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Aminophylline/氨茶碱 纯度/质量文件 产品仅供科研

货号:A594330 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

Aminophylline/氨茶碱 生物活性

靶点
  • PDE

    PDE, IC50:0.12 mM

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].

Aminophylline/氨茶碱 细胞实验

Cell Line
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

Aminophylline/氨茶碱 动物实验

Species
Animal Model
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

Aminophylline/氨茶碱 动物研究

Dose Mice: 10 mg/kg[3] (i.p.)
Administration i.p.

Aminophylline/氨茶碱 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
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 <<

Aminophylline/氨茶碱 参考文献

[1]Essayan DM. Cyclic nucleotide phosphodiesterases. J Allergy Clin Immunol. 2001 Nov;108(5):671-80.

[2]Daly JW, Jacobson KA, et al. Adenosine receptors: development of selective agonists and antagonists. Prog Clin Biol Res. 1987;230:41-63.

[3]Glass WF 2nd, Moore JB Jr. Inhibition of human lung cyclic GMP and cyclic AMP phosphodiesterases by certain nucleosides, nucleotides, and pharmacological phosphodiesterase inhibitors. Biochem Pharmacol. 1979 Apr 1;28(7):1107-12. doi: 10.1016/0006-2952(79)90313-7. PMID: 87197.

[4]Maniscalco WM, Wilson CM, Gross I. Influence of aminophylline and cyclic AMP on glycogen metabolism in fetal rat lung in organ culture. Pediatr Res. 1979 Dec;13(12):1319-22. doi: 10.1203/00006450-197912000-00003. PMID: 230447.

[5]Vohra MM. Effect of cyclic AMP, db-cyclic AMP and phosphodiesterase inhibitors on histamine inhibition of the contractile response of the mouse vas deferens. Agents Actions. 1984 Jan;14(1):11-20. doi: 10.1007/BF01966827. PMID: 6199954.

[6]Trembath PW, Shaw J. Potentiation of isoprenaline-induced plasma cyclic AMP response by aminophylline in normal and asthmatic subjects. Br J Clin Pharmacol. 1978 Dec;6(6):499-503. doi: 10.1111/j.1365-2125.1978.tb00873.x. PMID: 215179; PMCID: PMC1429697.

Aminophylline/氨茶碱 实验方案

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

Aminophylline/氨茶碱 技术信息

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

请根据您的动物给药指南选择适当的溶解方案。
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
方案 一
方案 二
方案 三
配制的工作液建议现用现配,短期内尽快用完。 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
方案 一
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