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Serlopitant

Cat. No. M9185
Serlopitant Structure
Synonym:

VPD-737; MK-0594

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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Serlopitant is a selective Neurokinin-1 (NK-1) receptor antagonist. Serlopitant (0.25 and 4 mg) significantly decreased the primary end point of daily micturitions but not the secondary end points compared with placebo. Serlopitant was generally well tolerated.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 555.53
Formula C29H28F7NO2
CAS Number 860642-69-9
Purity >98%
Solubility DMSO 10 mM
Storage at -20°C
References

A multicenter, double-blind, randomized, placebo controlled trial of a neurokinin-1 receptor antagonist for overactive bladder.
Frenkl TL, et al. J Urol. 2010 Aug;184(2):616-22. PMID: 20639026.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Serlopitant, VPD-737; MK-0594 supplier, Neurokinin Receptor, inhibitors

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