MIPS521
Based on 1 Customer Validation
MIPS521 is a positive allosteric modulator of adenosine A1 receptor (A1AR). MIPS521 also has a lower A1R allosteric affinity (pKB=4.95; KB=11 μM). MIPS521 exhibits pain-relieving effects in vivo through modulation of the increased levels of endogenous adenosine.
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: 98.21%
- CAS 番号: 1146188-19-3
- 分子式: C19H10ClF6NOS
- 分子量:449.80
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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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A1AR |
MIPS521 (compound 13o) (3-10 μM) improves the ability of R-PIA to promote A1AR-mediated ERK1/2 phosphorylation[1].
MIPS521 (0.3-30 μM; pretreament for 10 min, co-treatment for 30 min) produces a concentration-dependent potentiation of signalling by ADO in an inhibition of cAMP assay (expressed as a percentage of the inhibition of 3 μM forskolin-mediated cAMP) in CHO cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MIPS521 (10 μg in 10 μL; intrathecal administration) significantly reduces spontaneous pain in a conditioned place preference model[2].
MIPS521 (1-30 μg in 10 μL; intrathecal administration) reduces eEPSCs in spinal cord from nerve-injured rats, with a pEC50 of 6.9. The maximum MIPS521-induced decrease in synaptic current amplitude is significantly greater in nerve-injured rats than in sham surgery controls[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male and female Sprague-Dawley rats (7-12 weeks) were performed a partial nerve ligation (PNL) or sham surgery[2]
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Dosage:1, 3, 10, 30 μg in 10 μL
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Administration:Intrathecal administration
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Result:Reduced eEPSCs in spinal cord from nerve-injured rats and reversed mechanical hyperalgesia.
化学情報
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CAS 番号 1146188-19-3
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性状 Solid
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分子量 449.80
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分子式 C19H10ClF6NOS
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Color Light yellow to green yellow
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SMILES
O=C(C1=C(N)SC=C1C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)C3=CC=C(C=C3)Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 25 mg/mL (55.58 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. 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. 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 (276 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Aurelio L, et, al. Allosteric modulators of the adenosine A1 receptor: synthesis and pharmacological evaluation of 4-substituted 2-amino-3-benzoylthiophenes. J Med Chem. 2009 Jul 23;52(14):4543-7. [Content Brief]
[2]. Draper-Joyce CJ, et, al. Positive allosteric mechanisms of adenosine A 1 receptor-mediated analgesia. Nature. 2021 Sep;597(7877):571-576. [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. 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 | 2.2232 mL | 11.1161 mL | 22.2321 mL | 55.5803 mL |
| 5 mM | 0.4446 mL | 2.2232 mL | 4.4464 mL | 11.1161 mL | |
| 10 mM | 0.2223 mL | 1.1116 mL | 2.2232 mL | 5.5580 mL | |
| 15 mM | 0.1482 mL | 0.7411 mL | 1.4821 mL | 3.7054 mL | |
| 20 mM | 0.1112 mL | 0.5558 mL | 1.1116 mL | 2.7790 mL | |
| 25 mM | 0.0889 mL | 0.4446 mL | 0.8893 mL | 2.2232 mL | |
| 30 mM | 0.0741 mL | 0.3705 mL | 0.7411 mL | 1.8527 mL | |
| 40 mM | 0.0556 mL | 0.2779 mL | 0.5558 mL | 1.3895 mL | |
| 50 mM | 0.0445 mL | 0.2223 mL | 0.4446 mL | 1.1116 mL |
MIPS521 関連分類
HY-139644 関連分類
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