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BAY 59-3074

Cat. No. M8919
BAY 59-3074 Structure
Size Price Availability Quantity
10mg USD 80  USD80 In stock
25mg USD 150  USD150 In stock
50mg USD 240  USD240 In stock
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Quality Control & Documentation
Biological Activity

BAY-59-3074 is a novel cannabinoid CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors, respectively. BAY 59-3074 (0.3-3 mg/kg, p.o.) induce antihyperalgesic and antiallodynic effects against thermal or mechanical stimuli in rat models of chronic neuropathic. Antiallodynic efficacy of BAY 59-3074 (1 mg/kg, p.o.) in the spared nerve injury model was maintained after 2 weeks of daily administration. However, tolerance developed rapidly (within 5 days) for cannabinoid-related side effect. BAY 59-3074 have analgesic, antihyperalgesic, and antiallodynic properties in rat models of acute and chronic pain.

Chemical Information
Molecular Weight 453.36
Formula C18H13F6NO4S
CAS Number 406205-74-1
Solubility (25°C) DMSO: 30 mg/mL
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] Teng H, et al. Bioorg Med Chem Lett. Conformationally constrained analogs of BAY 59-3074 as novel cannabinoid receptor ligands.

[2] De Vry J, et al. J Pharmacol Exp Ther. 3-[2-cyano-3-(trifluoromethyl)phenoxy]phenyl-4,4,4-trifluoro-1-butanesulfonate (BAY 59-3074): a novel cannabinoid Cb1/Cb2 receptor partial agonist with antihyperalgesic and antiallodynic effects.

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