ONO-RS-082

Names

[ Name ]:
ONO-RS-082

[Synonym ]:
Ono-RS-082
C21H22ClNO3

Biological Activity

[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.

Chemical & Physical Properties

[ 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

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS09

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H410

[ Precautionary Statements ]:
P273-P501

[ RIDADR ]:
UN 3077 9 / PGIII

Articles

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

Toxins (Basel.) 3(9) , 1203-19, (2011)

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.

Traffic 11(12) , 1530-6, (2010)

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 (...

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.