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P2X3 antagonist 38

Cat. No. M42216
P2X3 antagonist 38 Structure
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Biological Activity

P2X3 antagonist 38 is a potent and orally active P2X3 antagonist with IC50 values of 0.132, 0.165, 0.421 µM for hP2X3, rP2X3, gpP2X3, respectively.

Chemical Information
Molecular Weight 478.47
Formula C22H25F3N6O3
CAS Number 2545974-71-6
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] Flavio Ewerton et al. Eur Urol Focus. Efficacy and Safety of Eliapixant in Overactive Bladder: The 12-Week, Randomised, Placebo-controlled Phase 2a OVADER Study

[2] Stefan Klein et al. Br J Clin Pharmacol. First-in-human study of eliapixant (BAY 1817080), a highly selective P2X3 receptor antagonist: Tolerability, safety and pharmacokinetics

[3] Lorcan P McGarvey et al. Lancet. Efficacy and safety of gefapixant, a P2X3 receptor antagonist, in refractory chronic cough and unexplained chronic cough (COUGH-1 and COUGH-2): results from two double-blind, randomised, parallel-group, placebo-controlled, phase 3 trials

[4] Alyn H Morice et al. Eur Respir J. The effect of gefapixant, a P2X3 antagonist, on cough reflex sensitivity: a randomised placebo-controlled study

[5] F Soto et al. Neuropharmacology. Antagonistic properties of the suramin analogue NF023 at heterologously expressed P2X receptors

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