| ONO-8130orally bioavailable antagonist of the prostaglandin E2 (PGE2) receptor EP |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
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- MSDS (Material Safety Data Sheet)
Chemical structure
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| Cas No. | 459841-96-4 | SDF | Download SDF |
| Chemical Name | 4-[[[2,3-dihydro-6-[(2-methylpropyl)[(4-methyl-2-thiazolyl)sulfonyl]amino]-1H-inden-5-yl]oxy]methyl]-benzoic acid | ||
| Canonical SMILES | OC(C1=CC=C(COC2=CC(CCC3)=C3C=C2N(S(C4=NC(C)=CS4)(=O)=O)CC(C)C)C=C1)=O | ||
| Formula | C25H28N2O5S2 | M.Wt | 500.6 |
| Solubility | ≤2mg/ml in ethanol;3mg/ml in DMSO;1mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
ONO-8130 is an orally bioavailable and selective antagonist of the prostaglandin E2 (PGE2) receptor EP1 with Ki value of 1.9 nM [1][2][3].
Prostaglandins contribute to the sensitization of peripheral and central nociceptive neurons during peripheral inflammation. Prostaglandin E2 (PGE2) is considered a dominant pronociceptive prostanoid. PGE2 receptors are G protein-coupled receptors and classified into 4 general subtypes (EP1, EP2, EP3, and EP4) that are located unevenly in different tissues. EP1 receptors play a major role in processing of pain [1].
In cystitis-related bladder pain mice, Oral preadministration of ONO-8130 at 0.3-30 mg/kg strongly prevented both the bladder pain-like behavior and referred hyperalgesia in a dose-dependent way. ONO-8130 at 30 mg/kg also reversed the established cystitis-related bladder pain. ONO-8130 also blocked prostaglandin E2 caused prompt phosphorylation of ERK in the L6 spinal cord [1]. In the guinea pig trachea (GPT), ONO-8130 inhibited the initial contraction mediated by PGE2. ONO-8130 also eliminated the spontaneous tone [2].
References:[1]. Miki T, Matsunami M, Nakamura S, et al. ONO-8130, a selective prostanoid EP1 receptor antagonist, relieves bladder pain in mice with cyclophosphamide-induced cystitis. Pain. 2011 Jun;152(6):1373-81.[2]. Sfholm J, Dahlén SE, Adner M. Antagonising EP1 and EP2 receptors reveal that the TP receptor mediates a component of antigen-induced contraction of the guinea pig trachea. Eur J Pharmacol. 2013 Oct 15;718(1-3):277-82.
