Bay 59-3074

SKU: orb1303876

Description

Bay 59-3074

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 406205-74-1
• MW: 453.36
• Purity: 97.68%
• Formula: C₁₈H₁₃F₆NO₄S
• SMILES: FC(F)(F)CCCS(=O)(=O)Oc1cccc(Oc2cccc(c2C#N)C(F)(F)F)c1
• Target: Cannabinoid Receptor
• Solubility: 10% DMSO+90% Corn Oil:2.5 mg/mL (5.51 mM);DMSO:50 mg/mL (110.29 mM)

Bioactivity

• Target IC50:
  CB2:45.5 nM(ki)|CB1:48.3nM(ki)
• In Vivo:
  In rat models of chronic neuropathic (chronic constriction injury, spared nerve injury, tibial nerve injury, and spinal nerve ligation models) and inflammatory pain (carrageenan and complete Freund's adjuvant models), BAY 59-3074 (0.3-3 mg/kg, p.o.) induced antihyperalgesic and antiallodynic effects against thermal or mechanical stimuli. 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 effects, which occur at doses above 1 mg/kg (e.g., hypothermia). Uptitration from 1 to 32 mg/kg p.o. (doubling of daily dose every 4th day) prevented the occurrence of such side effects, whereas antihyperalgesic and antiallodynic efficacy was maintained/increased. No withdrawal symptoms were seen after abrupt withdrawal following 14 daily applications of 1 to 10 mg/kg p.o.
• In Vitro:
  analgesic, antihyperalgesic, and antiallodynic properties in rat models of acute and chronic pain. The reference concentration is 10 μM.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CB1, CB, CB2, CannabinoidReceptor, Cannabinoid Receptor, Bay 59 3074, Bay 593074, Bay 59-3074, inhibit, Inhibitor

Compound Identifiers

PubChem CID

10479060