| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
IC50: 0.11 μM (leukotriene)[2]
Targets the 5-lipoxygenase (5-LOX) pathway in leukotriene biosynthesis. By inhibiting 5-LOX, Piriprost prevents the conversion of arachidonic acid to leukotriene A4 (LTA4) and subsequently to LTB4 and the cysteinyl leukotrienes (LTC4, LTD4, LTE4), key inflammatory mediators produced in leukocytes. |
|---|---|
| ln Vitro |
Piriprost potassium inhibits the release of both leukotrienes and histamine from isolated porcine lung cells, with an IC50 of 0.11 microM. It also increases alkaline phosphatase (ALP) activity in cultured endometrial stromal cells. Mode-of-action studies in cloned mouse mast cells confirm its role as an inhibitor of leukotriene formation.
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| ln Vivo |
Piriprost potassium (U-60257B) has been studied in various animal models of inflammation, including models of asthma, anaphylaxis, and contact dermatitis. By blocking leukotriene synthesis, it reduces airway constriction, vascular permeability, neutrophil infiltration, and tissue edema. It is typically administered parenterally or topically depending on the model.
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| Enzyme Assay |
Cell-free assays for 5-LOX inhibition are performed using purified human 5-LOX enzyme. The enzyme (0.5 microg) is incubated with arachidonic acid (50 microM), ATP (2 mM), CaCl2 (2 mM), and test compound at various concentrations in assay buffer (pH 7.4) for 10 min at 25degC. The reaction is stopped with cold methanol, and 5-HETE/leukotriene products are extracted and quantified by reverse-phase HPLC with UV detection at 235 nm.
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| Cell Assay |
Freshly isolated porcine lung cells are stimulated with calcium ionophore A23187 (5 microM) to trigger leukotriene and histamine release. Piriprost potassium is pre-incubated with cells for 15 min at 37degC. After 30 min stimulation, supernatants are collected. Leukotrienes (LTB4, LTC4, LTD4) are measured by enzyme immunoassay (EIA), and histamine is quantified by fluorometric assay after derivatization with o-phthalaldehyde.
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| Animal Protocol |
In mouse models of inflammation (e.g., contact hypersensitivity), animals receive topical or systemic administration of Piriprost potassium (1-10 mg/kg) prior to allergen challenge. Ear swelling is measured 24 h post-challenge. Skin biopsies are collected for myeloperoxidase activity and histology. In anaphylaxis models, serum histamine and leukotriene levels are measured after antigen challenge.
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| ADME/Pharmacokinetics |
Detailed PK data for Piriprost potassium is limited. As an inhibitor of leukotriene synthesis with modest molecular weight (463.65 g/mol), it is anticipated to have moderate oral bioavailability and a relatively short half-life in vivo. It has been used primarily as a topical or parenteral research tool rather than a systemically dosed drug candidate.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Piriprost potassium is not publicly available. As a 5-LOX inhibitor, it may have a similar safety profile to other leukotriene synthesis inhibitors, which can include potential gastrointestinal effects and drug-drug interactions when dosed systemically, though this compound is primarily used as a research tool.
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| References |
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| Additional Infomation |
See also: Piriprost (has active moiety).
Piriprost potassium (U 60257B) is a research chemical, not approved for human therapeutic use. It is a valuable tool for investigating the role of the 5-lipoxygenase pathway and leukotrienes in acute and chronic inflammatory conditions, asthma, allergic diseases, and eicosanoid metabolism. |
| Molecular Formula |
C26H34KNO4
|
|---|---|
| Molecular Weight |
463.65
|
| Exact Mass |
463.212
|
| CAS # |
88851-62-1
|
| PubChem CID |
23665631
|
| Appearance |
Typically exists as solid at room temperature
|
| Boiling Point |
618.6ºC at 760 mmHg
|
| Flash Point |
327.9ºC
|
| LogP |
3.438
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
32
|
| Complexity |
580
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
CCCCC[C@@H](/C=C/[C@@H]1C2=C(C[C@H]1O)N(C3=CC=CC=C3)C(=C2)CCCCC(=O)[O-])O.[K+]
|
| InChi Key |
UFJDMFZMRXDIKI-FFGYHVHASA-M
|
| InChi Code |
InChI=1S/C26H35NO4.K/c1-2-3-5-13-21(28)15-16-22-23-17-20(12-8-9-14-26(30)31)27(24(23)18-25(22)29)19-10-6-4-7-11-19;/h4,6-7,10-11,15-17,21-22,25,28-29H,2-3,5,8-9,12-14,18H2,1H3,(H,30,31);/q;+1/p-1/b16-15+;/t21-,22+,25+;/m0./s1
|
| Chemical Name |
potassium;5-[(4R,5R)-5-hydroxy-4-[(E,3S)-3-hydroxyoct-1-enyl]-1-phenyl-5,6-dihydro-4H-cyclopenta[b]pyrrol-2-yl]pentanoate
|
| 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 (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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1568 mL | 10.7840 mL | 21.5680 mL | |
| 5 mM | 0.4314 mL | 2.1568 mL | 4.3136 mL | |
| 10 mM | 0.2157 mL | 1.0784 mL | 2.1568 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.
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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