| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg | |||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
Pentosan Polysulfate is a potent and selective anti-HIV agent in vitro. It also targets inflammatory pathways, regulating NF-κB and reducing TNFα's proinflammatory effects, as well as reducing MCP-1 production triggered by high glucose. In the kidneys, it preserves renal function, lowers albuminuria, and lessens renal lesions, particularly tubulointerstitial inflammation.
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| ln Vitro |
Pentosan polysulfate inhibited HIV-1 activity at an ED50 of 0.19 μg/mL in MT-4 cells. It reduces HIV-1 antigen expression in HUT-78 cells with an ED50 of 0.02 μg/mL, and total suppression is achieved at 4.0 μg/mL [2]. Pentosan Polysulfate has been shown to regulate NF-κB, reduce TNFα's proinflammatory effects, and reduce MCP-1 production triggered by high glucose and advanced glycation end products (3).
In vitro, Pentosan Polysulfate demonstrates potent anti-HIV activity with an ED50 of 0.19 μg/mL in MT-4 cells. It also exhibits anti-inflammatory activity by regulating NF-κB and reducing TNFα's proinflammatory effects. It reduces MCP-1 production triggered by high glucose. These activities make it a compound of interest for research into HIV and inflammatory diseases. |
| ln Vivo |
In 5/6 nephrectomized rats, pentosan polysulfate has been demonstrated to reduce glomerulosclerosis and interstitial inflammation. Treatment with pentosan polysulfate preserves renal function, lowers albuminuria considerably, and lessens renal lesions, especially tubulointerstitial inflammation, greatly. In aged diabetic kidneys, pentosan polysulfate also lessens activation of proinflammatory genes and TNFα[3].
In vivo, Pentosan Polysulfate is used to treat interstitial cystitis and thrombi. It has been shown to preserve renal function, lower albuminuria considerably, and lessen renal lesions, especially tubulointerstitial inflammation, in aged diabetic kidneys. Its anti-inflammatory and anticoagulant activities contribute to its therapeutic effects. |
| Enzyme Assay |
The in vitro antiviral assay for Pentosan Polysulfate involves testing its activity against HIV-1 in MT-4 cells. Cells are infected with the virus and treated with varying concentrations of the compound. Viral replication is measured by assessing the production of viral proteins or by measuring the cytopathic effect. The ED50 is calculated from the dose-response curve.
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| Cell Assay |
In vitro cell culture studies for Pentosan Polysulfate utilize MT-4 cells to study its anti-HIV activity. Its anti-inflammatory effects can be studied in macrophage or endothelial cell lines. Cells are treated with the compound and stimulated with inflammatory triggers, and the production of cytokines and chemokines is measured by ELISA.
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| Animal Protocol |
In vivo animal experiments for Pentosan Polysulfate are performed in models of interstitial cystitis, thrombosis, and diabetic nephropathy. In the diabetic nephropathy model, the compound is administered, and renal function is assessed by measuring albuminuria and serum creatinine. Histopathological examination of kidney tissues is performed to evaluate renal lesions.
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| ADME/Pharmacokinetics |
Pentosan Polysulfate is a sulfated oligosaccharide with a molecular weight that varies depending on the source. It is a solid compound that is soluble in water. It is typically stored as a powder at -20°C for long-term stability. Its stability is maintained under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Toxicological data for Pentosan Polysulfate indicate that it is generally well-tolerated at therapeutic doses. Common side effects include gastrointestinal disturbances, headache, and hair loss. It has anticoagulant properties and can increase the risk of bleeding. It is contraindicated in patients with bleeding disorders or those taking anticoagulant medications.
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| Additional Infomation |
Pentosan Polysulfate is an approved drug for the treatment of interstitial cystitis in some countries. It is also used as an anticoagulant. It is not approved for the treatment of HIV. It is available as an oral formulation and as an injectable. Its anti-inflammatory and anticoagulant properties make it a compound of interest for research into various diseases.
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| CAS # |
9062-57-1
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| Related CAS # |
Pentosan Polysulfate Sodium (W/W 43%);140207-93-8
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| Appearance |
Off-white to light brown solid powder
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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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