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LY2828360

SKU: orb1299927

Description

LY2828360 is a potent and selective cannabinoid receptor 2 (CB2) agonist with a Ki of 40.3 nM. It demonstrates high functional selectivity for CB2 over CB1 (EC50 = 20.1 nM vs. >100,000 nM). This compound is a valuable research tool for studying CB2 receptor function in immunological and neurological contexts, both in vitro and in vivo.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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LY2828360

Key Properties

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CAS Number1231220-79-3
MW426.94
Purity99.51% (May vary between batches)
FormulaC22H27ClN6O
SMILESCN1CCN(CC1)c1nc(C)nc2n(C3CCOCC3)c(nc12)-c1ccccc1Cl
TargetCannabinoid Receptor
SolubilityDMSO:1 mg/mL (2.34 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.34 mM)

Bioactivity

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Target IC50
CB2:40.3 nM(Ki)
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.
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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.
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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CB, Cannabinoid Receptor, CannabinoidReceptor, inhibit, Inhibitor, LY2828360, LY-2828360, LY 2828360

Similar Products

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  • LY2828360

    LY2828360 [orb1220474]

    >98% (HPLC)

    1231220-79-3

    426.9

    C22H27ClN6O

    2 mg, 5 mg, 10 mg, 25 mg, 1 g, 500 mg, 200 mg, 100 mg, 50 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Compound Identifiers

PubChem CID
46833780 ↗

Key Properties

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No computed properties available.

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LY2828360 (orb1299927)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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2 mg
$ 80.00
5 mg
$ 90.00
10 mg
$ 120.00
25 mg
$ 190.00
50 mg
$ 260.00
100 mg
$ 360.00
200 mg
$ 510.00
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