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Pentoxifylline PDE inhibitor

Name: Pentoxifylline
Brand: Selleck Chemicals
SKU: S4345
Rating: 5 (2 reviews)

Cat.No.S4345

Pentoxifylline is a competitive nonselective phosphodiesterase inhibitor which raises intracellular cAMP, activates PKA, inhibits TNF and leukotriene synthesis, and reduces inflammation and innate immunity.

Chemical Structure

Molecular Weight: 278.31

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Quality Control

Batch: Purity: 99.82%

99.82

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Other PDE Inhibitors	Rolipram IBMX (3-Isobutyl-1-methylxanthine) Icariin Cilomilast Mardepodect (PF-2545920) Deltarasin PF-8380 Enpp-1-IN-1 Ibudilast BRL-50481

Chemical Information, Storage & Stability

Molecular Weight	278.31	Formula	C₁₃H₁₈N₄O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	6493-05-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(=O)CCCCN1C(=O)C2=C(N=CN2C)N(C1=O)C

Solubility

In vitro
Batch:

DMSO : 55 mg/mL (197.62 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 55 mg/mL

Ethanol : 55 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

In vitro	Pentoxifylline exhibits synergism with CDDP in killing MCF-7/E6 cells but does not affect sensitivity of the control cells. This compound inhibits G2 checkpoint function to a greater extent in MCF-7/E6 than in the parental cells. It acts primarily by increasing red blood cell deformability, by reducing blood viscosity and by decreasing the potential for platelet aggregation and thrombus formation. This chemical is efficacious in suppressing LPS-induced MO-derived TNF at the level of both TNF mRNA accumulation and TNF supernatant bioactivity. It (10 μM) suppresses the production of both biologically active TNF and TNF mRNA expression by more than 50% in LM cells. This agent blocks cachectin/TNF mRNA accumulation but has no effect upon the efficiency of reporter mRNA translation in RAW 264.7 macrophages. When combined with Dexamethasone, it causes a greater suppression of cachectin/TNF biosynthesis that can be achieved by either agent alone in RAW 264.7 macrophages.
In vivo	Pentoxifylline (500 mg) markedly inhibits increases in the serum levels of TNF and IL-6, as well as the effects on coagulation and fibrinolysis, in chimpanzees. This compound along with Endotoxin (4 ng/kg) also has a significant effect on thrombin generation in chimpanzees.
References	[1] https://pubmed.ncbi.nlm.nih.gov/7712469/ [2] https://pubmed.ncbi.nlm.nih.gov/3308412/ [3] https://pubmed.ncbi.nlm.nih.gov/2460096/ [4] https://pubmed.ncbi.nlm.nih.gov/2358784/ [5] https://pubmed.ncbi.nlm.nih.gov/8282778/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06344390	Recruiting	Cognitive Impairment	The First Hospital of Hebei Medical University	April 10 2024	Phase 1\|Phase 2
NCT06041932	Not yet recruiting	Liver Cirrhosis	Institute of Liver and Biliary Sciences India	November 1 2023	Not Applicable
NCT05490953	Recruiting	Hodgkin Lymphoma	University of Guadalajara\|Hospital Civil de Guadalajara	July 11 2022	Phase 4
NCT05189535	Completed	Breast Cancer Female\|Peripheral Neuropathy	Ain Shams University	October 3 2021	Phase 2\|Phase 3
NCT04152980	Recruiting	Neonatal Late Onset Sepsis	Erasmus Medical Center	January 12 2020	Phase 3
NCT05660694	Completed	Triamcinolone\|Pentoxifylline\|Vitamin E\|Oral Submucosa Fibrosis\|Tumor	Altamash Institute of Dental Medicine	January 1 2020	Phase 4

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