ONO-RS-082

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phospholipase

Research Areas >> Inflammation/Immunology

[In Vitro]

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]. Cell Viability Assay[3] Cell Line: A549 lung epithelial cell lines Concentration: 10 μM Incubation Time: 2-h pretreatment Result: Completely blocked HXA3-mediated PAO1-induced PMN transepithelial migration. Largely prevented PAO1-induced PGE2 release.

[In Vivo]

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]. Animal Model: MCT- pulmonary hypertension (PH) rat model[4] Dosage: 50 mg/kg/day Administration: Result: Reduced the development of PH in the MCT-PH model for long-term.

[References]

[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.

[ Density]:
1.247g/cm3

[ Boiling Point ]:
580.5ºC at 760mmHg

[ Molecular Formula ]:
C₂₁H₂₂ClNO₃

[ Molecular Weight ]:
371.85700

[ Flash Point ]:
304.9ºC

[ Exact Mass ]:
371.12900

[ PSA ]:
66.40000

[ LogP ]:
5.49580

[ Index of Refraction ]:
1.633

Click to get detail MSDS

[ Symbol ]:

GHS09

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H410

[ Precautionary Statements ]:
P273-P501

[ RIDADR ]:
UN 3077 9 / PGIII

Role of phospholipase A(2) in retrograde transport of ricin.

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Ricin is a protein toxin classified as a bioterror agent, for which there are no known treatment options available after intoxication. It is composed of an enzymatically active A-chain connected by a ...

A role for phospholipase A2 activity in membrane tubule formation and TGN trafficking.

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We have investigated the role of phospholipase A(2) (PLA(2) ) enzymes in generating membrane tubules at the trans-Golgi network (TGN). Constitutive TGN membrane tubules and those induced by over-expre...

Pyrimidine nucleotide-stimulated thromboxane A2 release from cultured glia.

Cell. Mol. Neurobiol. 18(5) , 477-86, (1998)

1. Uridine triphosphate (UTP), uridine diphosphate (UDP), cytidine triphosphate (CTP), and deoxythymidine triphosphate (TTP) caused concentration-dependent increases in the release of thromboxane A2 (...

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