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Sivopixant

Cat. No. M21200
Sivopixant Structure
Synonym:

S-600918

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Biological Activity

The P2X3 ligand-gated ion channel antagonist sivopixant (S-600918) is an oral phase II candidate compound for the study of refractory chronic cough.

Chemical Information
Molecular Weight 507.93
Formula C25H22ClN5O5
CAS Number 2414285-40-6
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] Lorcan McGarvey, et al. Lung. A Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Phase 2b Trial of P2X3 Receptor Antagonist Sivopixant for Refractory or Unexplained Chronic Cough

[2] Douglas S Burgoyne. Am J Manag Care. Managed care considerations for the treatment of chronic cough

[3] Akio Niimi, et al. Eur Respir J. Randomised trial of the P2X3 receptor antagonist sivopixant for refractory chronic cough

[4] Hiroyuki Kai, et al. Bioorg Med Chem Lett. Discovery of clinical candidate Sivopixant (S-600918): Lead optimization of dioxotriazine derivatives as selective P2X3 receptor antagonists

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Keywords: Sivopixant, S-600918 supplier, P2 Receptor, inhibitors, activators


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