ONO-8130 |
| Catalog No.GC14211 |
ONO-8130 est un antagoniste des récepteurs prostanoÏdes EP1 actif et sélectif par voie orale.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 459841-96-4
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 459841-96-4 | 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 |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9976 mL | 9.988 mL | 19.976 mL |
| 5 mM | 0.3995 mL | 1.9976 mL | 3.9952 mL |
| 10 mM | 0.1998 mL | 0.9988 mL | 1.9976 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)
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