| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
ONO-RS-082 targets phospholipase A2 (PLA2), an enzyme that releases fatty acids (like arachidonic acid) from the second carbon group of glycerol. This is a key step in the production of eicosanoids, which are potent inflammatory mediators. By inhibiting PLA2, ONO-RS-082 reduces the production of these inflammatory mediators.
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| ln Vitro |
Polymorphonuclear clear cells (PMNs) generated by P. aeruginosa strain PAO1 cannot migrate transepithelially when exposed to ONO-RS-082 (10 μM), suggesting that PLA2 is essential for this mechanism [3].
In vitro, ONO-RS-082 inhibits PLA2 with an IC50 of 1.0 µM. It is a reversible inhibitor. At a concentration of 3.5 µM, it has been shown to inhibit epinephrine-stimulated thromboxane production in human platelets. It can also interfere with endosomal tubule formation and Golgi complex maintenance. |
| ln Vivo |
ONO-RS-082 (50 mg/kg/day; prophylactic therapy, days 0 to 21) decreases the development of PH in the MCT-PH model with long-term activation of KCNK3 in vivo [4]. In contrast, short-term KCNK3 activation (curative treatment) in vivo by ONO-RS-082 failed to ameliorate PH symptoms, which was related to the total loss of KCNK3 expression in MCT-PH distribution from 14 to 21 days [4].
In vivo, ONO-RS-082 is used as a research tool to study inflammation and signal transduction. By inhibiting PLA2, it can reduce the production of inflammatory mediators in animal models. However, specific in vivo efficacy data are not detailed in the search results. |
| Enzyme Assay |
The in vitro enzyme inhibition assay for ONO-RS-082 measures its ability to inhibit PLA2 enzymatic activity. The assay is performed using purified PLA2 enzyme and a suitable substrate, such as a fluorescently labeled phospholipid. The release of the fluorescent product is monitored, and the IC50 is calculated from the inhibition curve.
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| Cell Assay |
Cell Viability Assay[3]
Cell Types: A549 lung epithelial cell line Tested Concentrations: 10 μM Incubation Duration: 2 hrs (hours) of pretreatment Experimental Results: Completely blocked HXA3-mediated PAO1-induced PMN transepithelial migration. PAO1-induced PGE2 release was largely prevented. In vitro cellular studies are conducted using various cell types, such as platelets. Cells are treated with ONO-RS-082, and its effects on eicosanoid production are measured. For example, the inhibition of epinephrine-stimulated thromboxane production in human platelets can be quantified by ELISA or other methods. |
| Animal Protocol |
Animal/Disease Models: MCT- Pulmonary Hypertension (PH) Rat Model [4]
Doses: 50 mg/kg/day Route of Administration: Experimental Results: Long-term reduction in the development of PH in the MCT-PH model. In vivo animal experiments for ONO-RS-082 are not detailed in the search results. However, as an inhibitor of PLA2, it could be used in models of inflammation. Animals would be administered the compound, and the levels of inflammatory mediators or the severity of inflammation would be assessed. |
| ADME/Pharmacokinetics |
ONO-RS-082 has a molecular formula of C21H22ClNO3 and a molecular weight of 371.86 g/mol. It is soluble in DMSO and ethanol. For research, it is typically stored at -20°C. Its purity is high for research-grade material (≥97%). It is a reversible inhibitor of Ca2+-independent PLA2.
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| Toxicity/Toxicokinetics |
As a research chemical, ONO-RS-082 is not intended for human use. Its toxicological profile is not fully characterized. Standard laboratory safety precautions should be followed. Its effects on inflammation are well-known from its mechanism of action.
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| References |
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| Additional Infomation |
ONO-RS-082 is a reversible inhibitor of phospholipase A2 used to study inflammation and lipid signaling. It is a valuable tool for dissecting the role of PLA2 and arachidonic acid metabolism in various biological processes. It is supplied as a high-purity research compound.
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| Molecular Formula |
C21H22NO3CL
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|---|---|
| Molecular Weight |
371.85728
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| Exact Mass |
371.129
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| CAS # |
99754-06-0
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| PubChem CID |
6438389
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| Appearance |
White to off-white solid powder
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| Density |
1.247g/cm3
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| Boiling Point |
580.5ºC at 760mmHg
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| Flash Point |
304.9ºC
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| Index of Refraction |
1.633
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| LogP |
5.495
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
26
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| Complexity |
486
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCC1=CC=C(C=C1)/C=C/C(=O)NC2=C(C=CC(=C2)Cl)C(=O)O
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| InChi Key |
MDVFITMPFHDRBZ-JLHYYAGUSA-N
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| InChi Code |
InChI=1S/C21H22ClNO3/c1-2-3-4-5-15-6-8-16(9-7-15)10-13-20(24)23-19-14-17(22)11-12-18(19)21(25)26/h6-14H,2-5H2,1H3,(H,23,24)(H,25,26)/b13-10+
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| Chemical Name |
4-chloro-2-[[(E)-3-(4-pentylphenyl)prop-2-enoyl]amino]benzoic acid
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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) |
DMSO : ~100 mg/mL (~268.92 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.72 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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. Solubility in Formulation 2: 2.5 mg/mL (6.72 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 | 2.6892 mL | 13.4459 mL | 26.8918 mL | |
| 5 mM | 0.5378 mL | 2.6892 mL | 5.3784 mL | |
| 10 mM | 0.2689 mL | 1.3446 mL | 2.6892 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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