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LY2828360

Catalog No. T7316   CAS 1231220-79-3

LY2828360 is a cannabinoid (CB) receptor 2 agonist (Ki = 40.3 nM). It selectively activates CB2 over CB1 in a GTPγS binding assay (EC50s = 20.1 and <100,000 nM, respectively).

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LY2828360 Chemical Structure
LY2828360, CAS 1231220-79-3
Pack Size Availability Price/USD Quantity
2 mg In stock $ 37.00
5 mg In stock $ 47.00
10 mg In stock $ 77.00
25 mg In stock $ 147.00
50 mg In stock $ 213.00
100 mg In stock $ 313.00
1 mL * 10 mM (in DMSO) In stock $ 52.00
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Purity: 98.61%
Purity: 98.45%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description LY2828360 is a cannabinoid (CB) receptor 2 agonist (Ki = 40.3 nM). It selectively activates CB2 over CB1 in a GTPγS binding assay (EC50s = 20.1 and >100,000 nM, respectively).
Targets&IC50 CB2:40.3 nM(Ki)
In vitro In vitro, LY2828360 was a slowly acting but efficacious G protein-biased CB2 agonist, inhibiting cAMP accumulation and activating extracellular signal-regulated kinase 1/2 signaling while failing to recruit arrestin, activate inositol phosphate signaling, or internalize CB2 receptors.
In vivo In wild-type (WT) mice, LY2828360 (3 mg/kg per day × 12 days) suppressed chemotherapy-induced neuropathic pain produced by paclitaxel without producing tolerance. Antiallodynic efficacy of LY2828360 was absent in CB2 knockout (KO) mice. Morphine (10 mg/kg per day × 12 days) tolerance developed in CB2KO mice but not in WT mice with a history of LY2828360 treatment (3 mg/kg per day × 12 days). LY2828360-induced antiallodynic efficacy was preserved in WT mice previously rendered tolerant to morphine (10 mg/kg per day × 12 days), but it was absent in morphine-tolerant CB2KO mice. Coadministration of LY2828360 (0.1 mg/kg per day × 12 days) with morphine (10 mg/kg per day × 12 days) blocked morphine tolerance in WT but not in CB2KO mice. WT mice that received LY2828360 coadministered with morphine exhibited a trend (P = 0.055) toward fewer naloxone-precipitated jumps compared with CB2KO mice. LY2828360 is a slowly signaling, G protein-biased CB2 agonist that attenuates chemotherapy-induced neuropathic pain without producing tolerance and may prolong effective opioid analgesia while reducing opioid dependence. LY2828360 may be useful as a first-line treatment in chemotherapy-induced neuropathic pain and may be highly efficacious in neuropathic pain states that are refractive to opioid analgesics.
Molecular Weight 426.94
Formula C22H27ClN6O
CAS No. 1231220-79-3

Storage

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

Solubility Information

DMSO: 20.83 mg/mL (48.79 mM)

TargetMolReferences and Literature

1. Lin X , Dhopeshwarkar A S , Huibregtse M , et al. The slowly signaling G protein-biased CB2 cannabinoid receptor agonist LY2828360 suppresses neuropathic pain with sustained efficacy and attenuates morphine tolerance and dependence[J]. Molecular Pharmacology, 2017:mol.117.109355.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Membrane Protein-targeted Compound Library Drug Repurposing Compound Library GPCR Compound Library Anti-Cancer Drug Library Anti-Fibrosis Compound Library Neuronal Signaling Compound Library Bioactive Compound Library Clinical Compound Library ReFRAME Related Library

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Keywords

LY2828360 1231220-79-3 GPCR/G Protein Cannabinoid Receptor Inhibitor LY 2828360 inhibit LY-2828360 inhibitor

 

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