Proxyphylline

Alias: NSC163343; NSC-163343; Monophylline; NSC 163343; Spasmolysin
Cat No.:V3125 Purity: ≥98%
Proxyphylline is a derivative of methylxanthine that is clinically used as a cardiac stimulant, a vasodilator and a bronchodilator.
Proxyphylline Chemical Structure CAS No.: 603-00-9
Product category: Adenosine Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Proxyphylline is a derivative of methylxanthine that is clinically used as a cardiac stimulant, a vasodilator and a bronchodilator. Proxyphylline acts by specifically opposing A2 adenosine receptors (Ki = 850 µM for platelets) in contrast to A1 adenosine receptors (Ki of 82 nM for the bovine brain). Vasodilatory and cardiac stimulatory effects have been observed with proxyphylline. It causes a clear positive inotropic effect along with an increase in coronary flow. Half-maximum relaxation of tracheal smooth muscle is achieved with 100 μg/mL of proxyphylline, which suppresses tracheal PDE-activity.

Biological Activity I Assay Protocols (From Reference)
Targets
A1 adenosine receptor
ln Vitro

In vitro activity: Proxyphylline has demonstrated heart-stimulating and vasodilatory effects. Proxyphylline has a clear positive inotropic effect and increases coronary flow[1]. Half-maximum relaxation of the smooth muscle in the trachea is achieved at 100 μg/mL of proxyphylline, which suppresses tracheal PDE-activity[2].

ln Vivo
Proxyphylline demonstrates bronchodilatory action[3]. In human lung tissue, proxyphylline inhibits the hydrolysis of cAMP and cGMP. Proxyphylline's apparent inhibition constant is 1.0 mM at high cAMP concentrations and 0.06–0.7 mM at low cAMP concentrations[3].
Animal Protocol


References

[1]. Effects of aminophylline, proxyphylline and a proxyphylline-Melilotus extract-rutin mixture(theoesberiven) on the heart and the coronary circulation. Jpn J Pharmacol. 1977 Oct;27(5):709-20.

[2]. Overadditive synergism between theophylline, diprophylline and proxyphylline in tracheal smooth muscle relaxation. Arzneimittelforschung. 1983;33(10):1450-4.

[3]. Pharmacokinetics and bronchodilatory effect of proxyphylline and theophylline. Eur J Respir Dis. 1984 Jan;65(1):20-7.

[4]. Inhibition of human lung cyclic nucleotide phosphodiesterases by proxyphylline, theophylline and their metabolites. Acta Pharmacol Toxicol (Copenh). 1982 Sep;51(3):250-2.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C10H14N4O3
Molecular Weight
238.25
Exact Mass
238.11
Elemental Analysis
C, 50.41; H, 5.92; N, 23.52; O, 20.15
CAS #
603-00-9
Related CAS #
603-00-9
Appearance
Solid powder
SMILES
CC(CN1C=NC2=C1C(=O)N(C(=O)N2C)C)O
InChi Key
KYHQZNGJUGFTGR-UHFFFAOYSA-N
InChi Code
InChI=1S/C10H14N4O3/c1-6(15)4-14-5-11-8-7(14)9(16)13(3)10(17)12(8)2/h5-6,15H,4H2,1-3H3
Chemical Name
7-(2-hydroxypropyl)-1,3-dimethylpurine-2,6-dione
Synonyms
NSC163343; NSC-163343; Monophylline; NSC 163343; Spasmolysin
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~47 mg/mL (~197.3 mM)
Water: N/A
Ethanol: N/A
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.49 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (10.49 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (10.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.1973 mL 20.9864 mL 41.9727 mL
5 mM 0.8395 mL 4.1973 mL 8.3945 mL
10 mM 0.4197 mL 2.0986 mL 4.1973 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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