Pentoxifylline

Alias: Dimethyloxohexylxanthine; EHT-0202, EHT0202, EHT 0202; BL 191, BL191, BL-191; Oxpentifylline, Pentoxifilina, Theobromine, Trental, Vazofirin, Etazolate
Cat No.:V3499 Purity: ≥98%
Pentoxifylline (also known as oxpentifylline, theobromine, dimethyloxohexylxanthine, EHT 0202, BL 191, BL-191; PTX, pentoxifilina, Trental), a xanthine derivative, is a nonselective PDE inhibitor used as a drug to treat muscle pain in people with peripheral artery disease.
Pentoxifylline Chemical Structure CAS No.: 6493-05-6
Product category: PDE
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
500mg
1g
2g
5g
10g
Other Sizes

Other Forms of Pentoxifylline:

  • Pentoxifylline-d6 (BL-191-d6; PTX-d6; Oxpentifylline-d6)
  • Pentoxifylline-d5 (BL-191-d5; PTX-d5; Oxpentifylline-d5)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Pentoxifylline (also known as oxpentifylline, theobromine, dimethyloxohexylxanthine, EHT 0202, BL 191, BL-191; PTX, pentoxifilina, Trental), a xanthine derivative, is a nonselective PDE inhibitor used as a drug to treat muscle pain in people with peripheral artery disease. It is generic and sold under many brand names worldwide. Its primary use in medicine is to reduce pain, cramping, numbness, or weakness in the arms or legs which occurs due to intermittent claudication, a form of muscle pain resulting from peripheral artery diseases. This is its only FDA, MHRA and TGA-labelled indication. However, pentoxifylline is also recommended for use off license as an adjunct to compression bandaging for the treatment of chronic venous leg ulcers by SIGN as this has been shown to improve healing rates

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Pentoxifylline suppresses cell growth in a dose-dependent manner (0.1–50 mM; 24-48 hours) [3]. In MDA-MB-231 cells, pentoxifylline (0.5 mM; 12-36 hours) decreases autophagy and promotes apoptosis [3]. In MDA-MB-231 cells, pentoxifylline (0.5 mM; 12-36 hours) promotes autophagy [3]. The G0/G1 phase of the cell cycle is blocked by pentoxifylline (0.5 mM; 24-48 hours) [3]. Elevated LC3-II/LC3 ratio is brought on by pentoxifylline [3].
ln Vivo
In rats exposed to transitory global ischemia, pentoxifylline (200 mg/kg; i.p.) exerts a protective effect and lessens cognitive damage [4].
Cell Assay
Cell proliferation assay[3]
Cell Types: MDA-MB-231 Cell
Tested Concentrations: 0.1 mM, 1 mM, 5 mM, 10 mM, 50 mM
Incubation Duration: 24 hrs (hours), 48 hrs (hours)
Experimental Results: Inhibition of cell proliferation in a dose-dependent manner.

Apoptosis analysis[3]
Cell Types: MDA-MB-231 Cell
Tested Concentrations: 0.5 mM
Incubation Duration: 12 hrs (hours), 24 hrs (hours), 36 hrs (hours)
Experimental Results: Induction of apoptosis.

Autophagy assay [3]
Cell Types: MDA-MB-231 Cell
Tested Concentrations: 0.5 mM
Incubation Duration: 24 hrs (hours), 48 hrs (hours)
Experimental Results: Approximately 20-28% of autophagy was induced.

Cell cycle analysis [3]
Cell Types: MDA-MB-231 Cell
Tested Concentrations: 0.5 mM
Incubation Duration: 24 hrs (hours), 48 hrs (hours)
Experimental Results: Induced G0/G1 phase arrest.

Western Blot Analysis[3]
Cell Types: MDA-MB-231 Cell
Tested Concentrations: 0.5 mM
Incubation Duration: 24 hrs (hours), 48 hrs (hours)
Experimental Results: Induction of high LC3-II/LC3 ratio.
Animal Protocol
Animal/Disease Models: Adult male Wistar rats, 12-13 weeks old (250-300 g) [4]
Doses: 200 mg/kg
Route of Administration: intraperitoneal (ip) injection, 1 hour before ischemia and 3 hrs (hrs (hours)) after ischemia.
Experimental Results: Significant Improves spatial memory and memory abilities. The effect was Dramatically different from that of the sham operation group and the vehicle group.
References
[1]. Iffat Hassan, et al. Pentoxifylline and its applications in dermatology. Indian Dermatol Online J. 2014 Oct-Dec; 5(4): 510–516.
[2]. A Ward, et al. Pentoxifylline. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic efficacy. Drugs. 1987 Jul;34(1):50-97.
[3]. Yessica Cristina Castellanos-Esparza, et al. Synergistic promoting effects of pentoxifylline and simvastatin on the apoptosis of triple-negative MDA-MB-231 breast cancer cells. Int J Oncol. 2018 Apr;52(4):1246-1254.
[4]. Shabnam Movassaghi, et al. Effect of Pentoxifylline on Ischemia- induced Brain Damage and Spatial Memory Impairment in Rat. Iran J Basic Med Sci. 2012 Sep-Oct; 15(5): 1083-1090.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C13H18N4O3
Molecular Weight
278.30702
CAS #
6493-05-6
Related CAS #
Pentoxifylline-d6;1185878-98-1;Pentoxifylline-d5;1185995-18-9
SMILES
c12c(n(c(=O)n(c1=O)CCCCC(C)=O)C)ncn2C
InChi Key
BYPFEZZEUUWMEJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C13H18N4O3/c1-9(18)6-4-5-7-17-12(19)10-11(14-8-15(10)2)16(3)13(17)20/h8H,4-7H2,1-3H3
Chemical Name
1,2,3,6-Tetrahydro-3,7-dimethyl-1-(5-oxohexyl)-2,6-purindion
Synonyms
Dimethyloxohexylxanthine; EHT-0202, EHT0202, EHT 0202; BL 191, BL191, BL-191; Oxpentifylline, Pentoxifilina, Theobromine, Trental, Vazofirin, Etazolate
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)
H2O : ~93.3 mg/mL (~335.24 mM)
DMSO : ≥ 2.8 mg/mL (~10.06 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 110 mg/mL (395.24 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.5931 mL 17.9656 mL 35.9312 mL
5 mM 0.7186 mL 3.5931 mL 7.1862 mL
10 mM 0.3593 mL 1.7966 mL 3.5931 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
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?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
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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