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Ro 51

Cat. No. M7209
Ro 51 Structure
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Biological Activity

Ro 51 is a potent, dual P2X3 and P2X2/3 antagonist (IC50 values are 2 and 5 nM for rP2X3 and hP2X2/3 respectively). Selective for P2X3 and P2X2/3 over other P2X receptors (IC50 values are > 10 μM for P2X1, P2X2, P2X4, P2X5, and P2X7). Cell permeable.

Chemical Information
Molecular Weight 474.29
Formula C17H23IN4O4
CAS Number 1050670-85-3
Solubility (25°C) DMSO 47.43 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Fryer and Maclagan. Naunyn Schmiedebergs Arch Pharmacol. Pancuronium and gallamine are antagonists for pre- and post-junctional muscarinic receptors in the guinea-pig lung.

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