CAS 99754-06-0|ONO-RS-082
| Common Name | ONO-RS-082 | ||
|---|---|---|---|
| CAS Number | 99754-06-0 | Molecular Weight | 371.85700 |
| Density | 1.247g/cm3 | Boiling Point | 580.5ºC at 760mmHg |
| Molecular Formula | C21H22ClNO3 | Melting Point | / |
| MSDS | ChineseUSA | Flash Point | 304.9ºC |
| Symbol | GHS09 | Signal Word | Warning |
Names
| Name | 4-chloro-2-[[(E)-3-(4-pentylphenyl)prop-2-enoyl]amino]benzoic acid |
|---|---|
| Synonym | More Synonyms |
ONO-RS-082 BiologicalActivity
| 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 >>PhospholipaseResearch 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 |
| InChIKey | MDVFITMPFHDRBZ-JLHYYAGUSA-N |
| SMILES | CCCCCc1ccc(C=CC(=O)Nc2cc(Cl)ccc2C(=O)O)cc1 |
Safety Information
| Symbol | GHS09 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H410 |
| Precautionary Statements | P273-P501 |
| RIDADR | UN 3077 9 / PGIII |
Articles23
More 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 (... |
Synonyms
| Ono-RS-082 |
| C21H22ClNO3 |
