Powder: -20°C for 3 years | In solvent: -80°C for 2 years
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).
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 20.83 mg/mL (48.79 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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LY2828360 1231220-79-3 GPCR/G Protein Cannabinoid Receptor Inhibitor inhibit LY-2828360 LY 2828360 inhibitor