99754-06-0

99754-06-0 structure

Name: ONO-RS-082
Chemical Name: 4-chloro-2-[[(E)-3-(4-pentylphenyl)prop-2-enoyl]amino]benzoic acid
CAS Number: 99754-06-0
Molecular Formula: C₂₁H₂₂ClNO₃
Molecular Weight: 371.85700
Catalog: Signaling Pathways Metabolic Enzyme/Protease Phospholipase
Create Date: 2018-12-30 07:23:16
Modify Date: 2024-01-05 19:03:04
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].

Name	4-chloro-2-[[(E)-3-(4-pentylphenyl)prop-2-enoyl]amino]benzoic acid
Synonyms	Ono-RS-082 C21H22ClNO3

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

Symbol	GHS09
Signal Word	Warning
Hazard Statements	H410
Precautionary Statements	P273-P501
RIDADR	UN 3077 9 / PGIII

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