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Chemical Structure : LY2828360
CAS No.: 1231220-79-3
Catalog No.: PC-47097Not For Human Use, Lab Use Only.
LY2828360 is a potent CB2 receptor agonist with similar affinity for human and rat CB2 receptors with Ki of 40.3 nM and 36.7 nM, respectively, shows EC50 of 20.1 nM in [35S]-GTPγS assays.
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| 10 mg | $198 | In stock | |
| 25 mg | $328 | In stock | |
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LY2828360 is a potent CB2 receptor agonist with similar affinity for human and rat CB2 receptors with Ki of 40.3 nM and 36.7 nM, respectively, shows EC50 of 20.1 nM in [35S]-GTPγS assays.
LY2828360 displays no agonist activity for CB1 receptor (EC50>10 uM).
LY2828360 is 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.
LY2828360 shows good CNS penetration and potent oral activity in a preclinical model of joint pain induced by intra-articular monoiodoacetic acid.
LY2828360 (0.3 mg/kg p.o.) produces a dose-related reversal of pain using incapacitance testing, demonstrating equivalent efficacy to the nonsteroidal anti-inflammatory drug diclofenac in the monoiodoacetic acid model.
| M.Wt | 426.949 | |
| Formula | C22H27ClN6O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
8-(2-chlorophenyl)-2-methyl-6-(4-methylpiperazin-1-yl)-9-(tetrahydro-2H-pyran-4-yl)-9H-purine |
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1. Lin X, et al. Mol Pharmacol. 2018 Feb;93(2):49-62.
2. Iyer V, et al. Eur J Pharmacol. 2020 Nov 5;886:173544.
3. Hollinshead SP, J Med Chem 56:5722–5733.
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