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MedKoo Cat#: 574833 | Name: ONO-RS-082
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

ONO-RS-082 is a reversible inhibitor of Ca2+-independent phospholipase A2. ONO-RS-082 may also disrupt endosome tubule formation and maintenance of the Golgi complex. Reduction in the potassium-channel current has been remedied by the application of the phospholipase inhibitor ONO-RS-082.

Chemical Structure

ONO-RS-082
ONO-RS-082
CAS#99754-06-0

Theoretical Analysis

MedKoo Cat#: 574833

Name: ONO-RS-082

CAS#: 99754-06-0

Chemical Formula: C21H22ClNO3

Exact Mass: 371.1288

Molecular Weight: 371.86

Elemental Analysis: C, 67.83; H, 5.96; Cl, 9.53; N, 3.77; O, 12.91

Price and Availability

Size Price Availability Quantity
25mg USD 530.00 2 Weeks
100mg USD 750.00 2 Weeks
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Related CAS #
No Data
Synonym
ONO-RS-082
IUPAC/Chemical Name
4-chloro-2-[[(2E)-1-oxo-3-(4-pentylphenyl)-2-propen-1-yl]amino]-benzoic acid
InChi Key
MDVFITMPFHDRBZ-JLHYYAGUSA-N
InChi Code
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+
SMILES Code
ClC1=CC(NC(/C=C/C2=CC=C(CCCCC)C=C2)=O)=C(C(O)=O)C=C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
ONO-RS-082 is an inhibitor of phospholipase A (PLA). ONO-RS-082 inhibits PLA2 with the IC50 of 1.0 μM.
In vitro activity:
This study examined whether cholinergic AA (arachidonic acid) acts as a second messenger in contraction of colonic circular muscle cells and if this role is altered by inflammation. Acetylcholine and the PLA(2) activator melittin induced cell contractions and AA release. Both effects were inhibited by the PLA(2) inhibitor ONO-RS-082. Cytosolic and membrane PLA(2) activities increased in response to acetylcholine. These were blocked by ONO-RS-082 and cytosolic PLA(2) 100-kilodalton antibody, but not by dithiothreitol, a secretory PLA(2) inhibitor. Reference: Gastroenterology. 2000 Jul;119(1):62-70. https://pubmed.ncbi.nlm.nih.gov/10889155/
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMF 33.0 88.74
DMSO 66.5 178.83
DMSO:PBS (pH 7.2) (1:3) 0.3 0.67
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 371.86 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Ali I, Campbell WB, Sarna SK. Impaired activation of cytosolic phospolipase A(2) in inflamed canine colonic circular muscle. Gastroenterology. 2000 Jul;119(1):62-70. doi: 10.1053/gast.2000.8558. PMID: 10889155. 2. Gailly P. Ca2+ entry in CHO cells, after Ca2+ stores depletion, is mediated by arachidonic acid. Cell Calcium. 1998 Oct;24(4):293-304. doi: 10.1016/s0143-4160(98)90053-7. PMID: 9883283.
In vitro protocol:
1. Ali I, Campbell WB, Sarna SK. Impaired activation of cytosolic phospolipase A(2) in inflamed canine colonic circular muscle. Gastroenterology. 2000 Jul;119(1):62-70. doi: 10.1053/gast.2000.8558. PMID: 10889155. 2. Gailly P. Ca2+ entry in CHO cells, after Ca2+ stores depletion, is mediated by arachidonic acid. Cell Calcium. 1998 Oct;24(4):293-304. doi: 10.1016/s0143-4160(98)90053-7. PMID: 9883283.
In vivo protocol:
TBD
1: Sousa D, Lima RT, Lopes-Rodrigues V, Gonzalez E, Royo F, Xavier CPR, Falcón- Pérez JM, Vasconcelos MH. Different Ability of Multidrug-Resistant and -Sensitive Counterpart Cells to Release and Capture Extracellular Vesicles. Cells. 2021 Oct 26;10(11):2886. doi: 10.3390/cells10112886. PMID: 34831110; PMCID: PMC8616370. 2: Cunningham KP, Holden RG, Escribano-Subias PM, Cogolludo A, Veale EL, Mathie A. Characterization and regulation of wild-type and mutant TASK-1 two pore domain potassium channels indicated in pulmonary arterial hypertension. J Physiol. 2019 Feb;597(4):1087-1101. doi: 10.1113/JP277275. Epub 2018 Nov 24. PMID: 30365877; PMCID: PMC6376074. 3: Bohnen MS, Roman-Campos D, Terrenoire C, Jnani J, Sampson KJ, Chung WK, Kass RS. The Impact of Heterozygous KCNK3 Mutations Associated With Pulmonary Arterial Hypertension on Channel Function and Pharmacological Recovery. J Am Heart Assoc. 2017 Sep 9;6(9):e006465. doi: 10.1161/JAHA.117.006465. PMID: 28889099; PMCID: PMC5634293. 4: Bhowmick R, Clark S, Bonventre JV, Leong JM, McCormick BA. Cytosolic Phospholipase A2α Promotes Pulmonary Inflammation and Systemic Disease during Streptococcus pneumoniae Infection. Infect Immun. 2017 Oct 18;85(11):e00280-17. doi: 10.1128/IAI.00280-17. PMID: 28808157; PMCID: PMC5649009. 5: Bechler ME, Brown WJ. Gβ1γ2 activates phospholipase A2-dependent Golgi membrane tubule formation. Front Cell Dev Biol. 2014 Feb 28;2(4):0004. doi: 10.3389/fcell.2014.00004. PMID: 25019068; PMCID: PMC4091998. 6: Ma L, Roman-Campos D, Austin ED, Eyries M, Sampson KS, Soubrier F, Germain M, Trégouët DA, Borczuk A, Rosenzweig EB, Girerd B, Montani D, Humbert M, Loyd JE, Kass RS, Chung WK. A novel channelopathy in pulmonary arterial hypertension. N Engl J Med. 2013 Jul 25;369(4):351-361. doi: 10.1056/NEJMoa1211097. PMID: 23883380; PMCID: PMC3792227. 7: Anderson M, Kim EY, Hagmann H, Benzing T, Dryer SE. Opposing effects of podocin on the gating of podocyte TRPC6 channels evoked by membrane stretch or diacylglycerol. Am J Physiol Cell Physiol. 2013 Aug 1;305(3):C276-89. doi: 10.1152/ajpcell.00095.2013. Epub 2013 May 8. PMID: 23657570. 8: Klokk TI, Lingelem AB, Myrann AG, Sandvig K. Role of phospholipase A(2) in retrograde transport of ricin. Toxins (Basel). 2011 Sep;3(9):1203-19. doi: 10.3390/toxins3091203. Epub 2011 Sep 23. PMID: 22069763; PMCID: PMC3202871. 9: Wormser C, Pore SA, Elperin AB, Silverman LN, Light DB. Potentiation of regulatory volume decrease by a p2-like receptor and arachidonic acid in american alligator erythrocytes. J Membr Biol. 2011 Jul;242(2):75-87. doi: 10.1007/s00232-011-9377-3. Epub 2011 Jul 5. PMID: 21728043. 10: Wormser C, Mason LZ, Helm EM, Light DB. Regulatory volume response following hypotonic stress in Atlantic salmon erythrocytes. Fish Physiol Biochem. 2011 Dec;37(4):745-59. doi: 10.1007/s10695-011-9474-3. Epub 2011 Feb 19. PMID: 21336592. 11: Schmidt JA, Kalkofen DN, Donovan KW, Brown WJ. A role for phospholipase A2 activity in membrane tubule formation and TGN trafficking. Traffic. 2010 Dec;11(12):1530-6. doi: 10.1111/j.1600-0854.2010.01115.x. Epub 2010 Sep 28. PMID: 20874826; PMCID: PMC4906538. 12: Macianskiene R, Gwanyanya A, Sipido KR, Vereecke J, Mubagwa K. Induction of a novel cation current in cardiac ventricular myocytes by flufenamic acid and related drugs. Br J Pharmacol. 2010 Sep;161(2):416-29. doi: 10.1111/j.1476-5381.2010.00901.x. PMID: 20735425; PMCID: PMC2989592. 13: Lee OR, Kim SJ, Kim HJ, Hong JK, Ryu SB, Lee SH, Ganguly A, Cho HT. Phospholipase A(2) is required for PIN-FORMED protein trafficking to the plasma membrane in the Arabidopsis root. Plant Cell. 2010 Jun;22(6):1812-25. doi: 10.1105/tpc.110.074211. Epub 2010 Jun 4. PMID: 20525850; PMCID: PMC2910968. 14: Judson BL, Brown WJ. Assembly of an intact Golgi complex requires phospholipase A2 (PLA2) activity, membrane tubules, and dynein-mediated microtubule transport. Biochem Biophys Res Commun. 2009 Nov 20;389(3):473-7. doi: 10.1016/j.bbrc.2009.08.173. Epub 2009 Sep 9. PMID: 19747452; PMCID: PMC2764284. 15: Doody AM, Antosh AL, Brown WJ. Cytoplasmic phospholipase A2 antagonists inhibit multiple endocytic membrane trafficking pathways. Biochem Biophys Res Commun. 2009 Oct 30;388(4):695-9. doi: 10.1016/j.bbrc.2009.08.067. Epub 2009 Aug 18. PMID: 19695219; PMCID: PMC2764267. 16: DalBó S, Goulart S, Horst H, Pizzolatti MG, Ribeiro-do-Valle RM. Activation of endothelial nitric oxide synthase by proanthocyanidin-rich fraction from Croton celtidifolius (Euphorbiaceae): involvement of extracellular calcium influx in rat thoracic aorta. J Pharmacol Sci. 2008 Jun;107(2):181-9. doi: 10.1254/jphs.fp0072385. PMID: 18566521. 17: Pajor AM, Randolph KM. Inhibition of the Na+/dicarboxylate cotransporter by anthranilic acid derivatives. Mol Pharmacol. 2007 Nov;72(5):1330-6. doi: 10.1124/mol.107.035352. Epub 2007 Aug 22. PMID: 17715401. 18: Hurley BP, Williams NL, McCormick BA. Involvement of phospholipase A2 in Pseudomonas aeruginosa-mediated PMN transepithelial migration. Am J Physiol Lung Cell Mol Physiol. 2006 Apr;290(4):L703-L709. doi: 10.1152/ajplung.00390.2005. Epub 2005 Nov 4. PMID: 16272174. 19: Randriamboavonjy V, Kiss L, Falck JR, Busse R, Fleming I. The synthesis of 20-HETE in small porcine coronary arteries antagonizes EDHF-mediated relaxation. Cardiovasc Res. 2005 Feb 1;65(2):487-94. doi: 10.1016/j.cardiores.2004.10.029. PMID: 15639488. 20: Islam A, Sakamoto Y, Kosaka K, Yoshitome S, Sugimoto I, Yamada K, Shibuya E, Vande Woude GF, Hashimoto E. The distinct stage-specific effects of 2-(p-amylcinnamoyl)amino-4-chlorobenzoic acid on the activation of MAP kinase and Cdc2 kinase in Xenopus oocyte maturation. Cell Signal. 2005 Apr;17(4):507-23. doi: 10.1016/j.cellsig.2004.09.011. PMID: 15601628.

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