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Bay 59-3074

Catalog No. T3699   CAS 406205-74-1

Bay 59-3074 is a CB1/CB2 receptor partial agonist (Ki: 48.3/45.5 nM). In rat models of chronic neuropathic and inflammatory pain, it displays anti-hyperalgesic and antiallodynic properties.

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Bay 59-3074 Chemical Structure
Bay 59-3074, CAS 406205-74-1
Pack Size Availability Price/USD Quantity
5 mg In stock $ 39.00
10 mg In stock $ 64.00
25 mg In stock $ 122.00
50 mg In stock $ 198.00
100 mg In stock $ 369.00
200 mg In stock $ 549.00
1 mL * 10 mM (in DMSO) In stock $ 43.00
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Purity: 99.69%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Bay 59-3074 is a CB1/CB2 receptor partial agonist (Ki: 48.3/45.5 nM). In rat models of chronic neuropathic and inflammatory pain, it displays anti-hyperalgesic and antiallodynic properties.
Targets&IC50 CB1:48.3nM(ki), CB2:45.5 nM(ki)
In vitro analgesic, antihyperalgesic, and antiallodynic properties in rat models of acute and chronic pain. The reference concentration is 10 μM.
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.
Molecular Weight 453.36
Formula C18H13F6NO4S
CAS No. 406205-74-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (110.29 mM)

TargetMolReferences and Literature

1. De Vry J, et al. J Pharmacol Exp Ther. 2004 Aug;310(2):620-32. 2. De Vry J, et al. Eur J Pharmacol. 2004 Nov 28;505(1-3):127-33.

TargetMolCitations

1. Xu C, Zhou Y, Liu Y, et al.Specific pharmacological and Gi/o protein responses of some native GPCRs in neurons.Nature Communications.2024, 15(1): 1990.

Related compound libraries

This product is contained In the following compound libraries:
ReFRAME Related Library NO PAINS Compound Library GPCR Compound Library Neuronal Signaling Compound Library Immunology/Inflammation Compound Library Bioactive Compound Library Fluorochemical Library Anti-Obesity Compound Library Anti-Fibrosis Compound Library Bioactive Compounds Library Max

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Keywords

Bay 59-3074 406205-74-1 GPCR/G Protein Cannabinoid Receptor inhibit Inhibitor Bay 593074 Bay 59 3074 inhibitor

 

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