For research use only. Not for therapeutic Use.
ONO-RS-082 is an inhibitor of phospholipase A (PLA)[1]. ONO-RS-082 inhibits PLA2 with the IC50 of 1.0 μM, but does not inhibit PLC even at 100 μM[2].
ONO-RS-082 (10 μM) prevents P. aeruginosa strain PAO1-induced polymorphonumclear cells (PMNs) transepithelial migration, demonstrating that PLA2 activity is crucial to this process[3].
In vivo long-term activation of KCNK3 by ONO-RS-082 (50 mg/kg/day; preventive treatment, day 0 to day 21) reduces the development of PH in the MCT-PH model[4].
In contrast, in vivo short-term KCNK3 activation by ONO-RS-082 (curative treatment) fails to reduce PH symptoms, which is attributed to the complete loss of KCNK3 expression in MCT-PH rats at days 14 to 21[4].
| Catalog Number | I011738 |
| CAS Number | 99754-06-0 |
| Synonyms | 4-chloro-2-[[(E)-3-(4-pentylphenyl)prop-2-enoyl]amino]benzoic acid |
| Molecular Formula | C21H22ClNO3 |
| Purity | ≥95% |
| InChI | 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+ |
| InChIKey | MDVFITMPFHDRBZ-JLHYYAGUSA-N |
| SMILES | CCCCCC1=CC=C(C=C1)C=CC(=O)NC2=C(C=CC(=C2)Cl)C(=O)O |
| Reference | [1]. H S Banga,et al. Activation of phospholipases A and C in human platelets exposed to epinephrine: role of glycoproteins IIb/IIIa and dual role of epinephrine. Proc Natl Acad Sci U S A.1986 Dec;83(23):9197-201. [2]. H Ohno, et al. Effect of phospholipase A2 inhibitors on mouse T lymphocytes. I. Phospholipase A2 inhibitors exert similar immunological activities as glycosylation inhibiting factor. Int Immunol. 1989;1(4):425-33. [3]. Bryan P Hurley, et al. Selective eicosanoid-generating capacity of cytoplasmic phospholipase A2 in Pseudomonas aeruginosa-infected epithelial cells. Am J Physiol Lung Cell Mol Physiol. 2011 Feb;300(2):L286-94. [4]. Hélène Le Ribeuz, et al. Implication of Potassium Channels in the Pathophysiology of Pulmonary Arterial Hypertension. Biomolecules. 2020 Sep 1;10(9):1261. |
