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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 1050670-85-3
- Formel: C17H23IN4O4
- Molecular Weight:474.29
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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
Chemical Information
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CAS. Nr. 1050670-85-3
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Molecular Weight 474.29
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Ro-51 Related Classifications
HY-14485 Related Classifications
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