Ro-51
Ro-51 is a potent and selective dual P2X3/P2X2/3 antagonist, with IC50 of 2 nM and 5 nM for P2X3 and P2X2/3, respectively. Ro-51 can be used for the research for pain.
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。
- CAS 番号: 1050670-85-3
- 分子式: C17H23IN4O4
- 分子量:474.29
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
P2X 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
IC50: 2 nM (P2X3), 5 nM (P2X2/3)[1]
Ro-51 has highly selective for P2X 3 and P2X 2/3 exhibiting no antagonistic activity at other P2X receptor family members tested (P2X 1 , P2X 2 , P2X 4 , P2X 5 , and P2X 7 ) at concentrations up to 10 μM[1].
RO51 also shows a significant drop in potency on human P2X3 receptors (IC50 = 110.5 and 0.04 nM, respectively for human and rat P2X3)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rat[1]
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Dosage:2 mg/kg (Pharmacokinetic Analysis)
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Administration:Oral administration
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Result:AUC= 237 ng/h/mL, T 1/2 =1.52 h
化学情報
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CAS 番号 1050670-85-3
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分子量 474.29
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分子式 C17H23IN4O4
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SMILES
OCC(NC1=NC=C(OC2=CC(I)=C(OC)C=C2C(C)C)C(N)=N1)CO
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Alam Jahangir,et al. Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1632-5. [Content Brief]
[2]. Alexandre Serrano, et al. Differential Expression and Pharmacology of Native P2X Receptors in Rat and Primate Sensory Neurons. J Neurosci. 2012 Aug 22; 32(34): 11890–11896. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)