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Rac-Modipafant

Cat. No. M9659
Rac-Modipafant Structure
Synonym:

Modipafant racemate; UK-74505

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Biological Activity

Rac-Modipafant (UK-74505) is an orally active, selective, long-acting irreversible platelet activating factor receptor (PAFR) antagonist.

Chemical Information
Molecular Weight 605.09
Formula C34H29ClN6O3
CAS Number 122956-68-7
Solubility (25°C) Soluble in HCl 0.1%
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] Ana T Guerrero, et al. Naunyn Schmiedebergs Arch Pharmacol. The role of PAF/PAFR signaling in zymosan-induced articular inflammatory hyperalgesia

[2] Danielle G Souza, et al. Proc Natl Acad Sci U S A. Essential role of platelet-activating factor receptor in the pathogenesis of Dengue virus infection

[3] M J Parry, et al. J Lipid Mediat Cell Signal. Pharmacological profile of UK-74,505, a novel and selective PAF antagonist with potent and prolonged oral activity

[4] V A Alabaster, et al. Agents Actions Suppl. UK-74,505, a novel and selective PAF antagonist, exhibits potent and long lasting activity in vivo

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Keywords: Rac-Modipafant, Modipafant racemate; UK-74505 supplier, Platelet-activating Factor Receptor, inhibitors, activators


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