Proxyphylline
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Ki: 82 nM for bovine brain A1 adenosine receptor
Proxyphylline is an A1 adenosine receptor antagonist.
The A1 adenosine receptor, the best characterized purinergic receptor family, can mediate responses via multiple pertussis toxin-sensitive GTP binding proteins to various different effectors.
In vitro: Previous study showed that proxyphylline could selectively antagonize A1 adenosine receptors versus A2 adenosine receptors (Ki = 850 μM for platelets) [1].
In vivo: In a previous study, rats that were allodynic following the vincristine injections were randomly allocated into four groups. Theoesberiven F (a combination of proxyphylline and Melilotus extract) was administered to rats. Results showed that the decreased paw withdrawal threshold induced by vincristine injection was increased by theoesberiven F treatment and the increased withdrawal frequency to cold stimuli was also reduced by theoesberiven F treatment [2].
Clinical trial: The proxyphylline PK was measured in healthy adults after intravenous, single oral and multiple oral doses to produce steady state. The mean peak time after oral administration was 29 min. The apparent volume of distribution was 0.611/kg. The ranges of biological half-life were 8.1-12.1 h and 8.3-12.6 h calculated from serum and urine data, respectively. In additioin, 24% of the dose was excreted in urine, which agreed with the relationship between the calculated total body clearance and the renal clearance of the drug [3].
References:
[1] U. Schwabe, D. Ukena and M. J. Lohse. Xanthine derivatives as antagonists at A1 and A2 adenosine receptors. Naunyn-Schmiedeberg's Arch.Pharmacol. 330,212-221 (1985).
[2] S. Bang, Y. S. Kim and S. R. Jeong. Anti-allodynic effect of theoesberiven F in a vincristine-induced neuropathy model. Exp. Ther. Med. 12(2), 799-803 (2016).
[3] Selvig K. Pharmacokinetics of proxyphylline in adults after intravenous and oral administration. Eur J Clin Pharmacol. 1981 Jan;19(2):149-55.
Storage | Store at -20°C |
M.Wt | 238.2 |
Cas No. | 603-00-9 |
Formula | C10H14N4O3 |
Synonyms | NSC 163343 |
Solubility | ≥10.1 mg/mL in DMSO; ≥22.77 mg/mL in EtOH with ultrasonic; ≥26.5 mg/mL in H2O |
Chemical Name | 3,7-dihydro-7-(2-hydroxypropyl)-1,3-dimethyl-1H-purine-2,6-dione |
SDF | Download SDF |
Canonical SMILES | CN(C(N1C)=O)C2=C(N(CC(O)C)C=N2)C1=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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