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S-777469 

Cat. No. M30812
S-777469  Structure
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Biological Activity

S-777469 is a selective and orally available cannabinoid type 2 receptor (CB2) agonist with a Ki of 36 nM. S-777469 significantly suppresses compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 produces its antipruritic effects by inhibiting itch signal transmission through CB2 agonism.

Chemical Information
Molecular Weight 414.47
Formula C23H27FN2O4
CAS Number 885496-53-7
Form Solid
Solubility (25°C) DMSO 83.33 mg/mL (ultrasonic)
Storage 4°C, protect from light
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] Takayo Haruna, et al. Pharmacology. The Inhibitory Effect of S-777469, a Cannabinoid Type 2 Receptor Agonist, on Skin Inflammation in Mice

[2] Takayo Haruna, et al. Pharmacology. S-777469, a novel cannabinoid type 2 receptor agonist, suppresses itch-associated scratching behavior in rodents through inhibition of itch signal transmission

[3] Kazutaka Sekiguchi, et al. Xenobiotica. The metabolism and pharmacokinetics of [14C]-S-777469, a new cannabinoid receptor 2 selective agonist, in healthy human subjects

[4] Kazutaka Sekiguchi, et al. Xenobiotica. Non-clinical evaluation of the metabolism, pharmacokinetics and excretion of S-777469, a new cannabinoid receptor 2 selective agonist

[5] Masahide Odan, et al. Bioorg Med Chem Lett. Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent

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