| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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ONO-RS-082 is a novel, potent and reversible inhibitor of Ca2+-independent phospholipase A2. At 3.5 µM, it has been shown to inhibit epinephrine-stimulated thromboxane production in human platelets. ONO-RS-082 can also disrupt endosome tubule formation and maintenance of the Golgi complex.
| 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].
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|---|---|
| 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].
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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. |
| 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. |
| References |
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| Molecular Formula |
C21H22NO3CL
|
|---|---|
| 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+
|
| 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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