ONO-8711 |
| カタログ番号GC16027 |
ONO-8711 は、EP1 受容体の強力かつ選択的な競合的アンタゴニストです (Ki = ヒトおよびマウスの EP1 に対してそれぞれ 0.6 および 1.7 nM)。 ONO-8711 は、結腸癌、乳癌、および口腔癌のマウスモデルにおいて、腫瘍の発生率と多重度を効果的に低下させます。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 216158-34-8
Sample solution is provided at 25 µL, 10mM.
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ONO-8711 is a novel and selective EP1 antagonist.
Prostaglandin (PG) E2 functions by acting on a group of G-protein-coupled receptors (GPCRs) EP receptros. The EP receptors exhibit differences in signal transduction, tissue localization, and regulation of expression. The EP receptors have been implicated in various physiological and pathophysiological functions [2].
In vitro: In human pulmonary vessels, ONO-8711 (30 μM) non-competitively blocked the contractions produced with sulprostone, an EP1,3 agonist [3].
In vivo: In azoxymethane-treated C57BL/6J mice, administration of 250, 500, or 1000 ppm of ONO-8711 dose-dependently reduced ACF formation. In Min mice with a nonsense mutation in the adenomatous polyposis coli gene, treatment with 500 ppm ONO-8711 significantly reduced the number of intestinal polyps [1]. In female SD rats given PhIP, administration of ONO-8711 at 400 or 800 p.p.m. delayed occurrence of breast tumors for 2 or 4 weeks, respectively [4]. Treatment with ONO-8711 (800 p.p.m.) significantly decreased PhIP-induced breast cancer incidence, multiplicity and volume when compared with those of control rats [4].
References:
[1] Watanabe K, Kawamori T, Nakatsugi S, et al. Role of the prostaglandin E receptor subtype EP1 in colon carcinogenesis[J]. Cancer research, 1999, 59(20): 5093-5096.
[2] Sugimoto Y, Narumiya S. Prostaglandin E receptors[J]. Journal of Biological Chemistry, 2007, 282(16): 11613-11617.
[3] Norel X, de Montpreville V, Brink C. Vasoconstriction induced by activation of EP 1 and EP 3 receptors in human lung: effects of ONO-AE-248, ONO-DI-004, ONO-8711 or ONO-8713[J]. Prostaglandins & other lipid mediators, 2004, 74(1): 101-112.
[4] Kawamori T, Uchiya N, Nakatsugi S, et al. Chemopreventive effects of ONO-8711, a selective prostaglandin E receptor EP1 antagonist, on breast cancer development[J]. Carcinogenesis, 2001, 22(12).
| Cas No. | 216158-34-8 | SDF | |
| Chemical Name | 6-[(2R,3S)-3-[[[(4-chloro-2-methylphenyl)sulfonyl]amino]methyl]bicyclo[2.2.2]oct-2-yl]-5Z-hexenoic acid | ||
| Canonical SMILES | ClC1=CC(C)=C(S(N([H])C[C@@H](C2CCC3CC2)[C@H]3/C=C\CCCC(O)=O)(=O)=O)C=C1 | ||
| Formula | C22H30ClNO4S | M.Wt | 439.2 |
| 溶解度 | ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/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 | 2.2769 mL | 11.3843 mL | 22.7687 mL |
| 5 mM | 0.4554 mL | 2.2769 mL | 4.5537 mL |
| 10 mM | 0.2277 mL | 1.1384 mL | 2.2769 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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 14 reference(s) in Google Scholar.)
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