MRS1220
Based on 1 Customer Validation
MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a Ki of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system. MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.52%
- CAS 番号: 183721-15-5
- 分子式: C21H14ClN5O2
- 分子量:403.82
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Adenosine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
7.2 nM
Compound: 42, MRS1220
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Antagonist activity at human adenosine A3 receptor expressed in CHO cells by [S35]GTPgammaS binding assay
Antagonist activity at human adenosine A3 receptor expressed in CHO cells by [S35]GTPgammaS binding assay
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[PMID: 22468757] |
| HCT-116 | IC50 |
>10 μM
Compound: MRS1220
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Cytotoxicity against human HCT-116 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay
Cytotoxicity against human HCT-116 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay
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[PMID: 35707146] |
| PC-3 | IC50 |
>10 μM
Compound: MRS1220
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Cytotoxicity against human PC-3 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay
Cytotoxicity against human PC-3 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay
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[PMID: 35707146] |
| WI-38 | IC50 |
>10 μM
Compound: MRS1220
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Cytotoxicity against human WI-38 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay
Cytotoxicity against human WI-38 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay
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[PMID: 35707146] |
MRS 1220 reverses the effect of A3 agonist-elicited inhibition of tumor necrosis factor-α formation in the human macrophage U-937 cell line with an IC50 of 0.3 μM[1].
VEGF secretion in U87MG glioblastoma stem-like cells (GSCs) decreases ~25% with MRS1220 after 72 h of hypoxia[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U87MG GSCs
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Concentration:10 μM
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Incubation Time:72 hours
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Result:Decreased ~25% VEGF secretion.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Eight, 8 week-old male Sprague-Dawley rats bearing C6 (GSCs)[2]
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Dosage:0.15 mg/kg/72 h
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Administration:Administered by intraperitoneal inoculation, for fifteen days
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Result:A reduction close to 80% and 90% in tumor volume compared to the vehicle-treated group at day ten and fifteen post-treatment, respectively.
化学情報
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CAS 番号 183721-15-5
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性状 Solid
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分子量 403.82
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分子式 C21H14ClN5O2
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Color White to off-white
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SMILES
O=C(NC1=NC2=C(C=C(Cl)C=C2)C3=NC(C4=CC=CO4)=NN13)CC5=CC=CC=C5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
DMSO : 4 mg/mL (9.91 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (277 KB)
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SDS (252 KB)
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- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. K A Jacobson, et al. Pharmacological characterization of novel A3 adenosine receptor-selective antagonists. Neuropharmacology. 1997 Sep;36(9):1157-65. [Content Brief]
[2]. René Rocha, et al. The Adenosine A₃ Receptor Regulates Differentiation of Glioblastoma Stem-Like Cells to Endothelial Cells under Hypoxia. Int J Mol Sci. 2018 Apr 18;19(4):1228. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4764 mL | 12.3818 mL | 24.7635 mL | 61.9088 mL |
| 5 mM | 0.4953 mL | 2.4764 mL | 4.9527 mL | 12.3818 mL |
MRS1220 関連分類
HY-103190 関連分類
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