ONO-8130
目录号 : GC14211
A selective, orally bioavailable EP1 antagonist
Cas No.:459841-96-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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 | |
| 化学名 | 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 | ||
| 分子式 | C25H28N2O5S2 | 分子量 | 500.6 |
| 溶解度 | ≤2mg/ml in ethanol;3mg/ml in DMSO;1mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。