Basic information Safety Supplier Related

LY2828360

Basic information Safety Supplier Related

LY2828360 Basic information

Product Name:
LY2828360
Synonyms:
  • LY2828360
  • 8-(2-chlorophenyl)-2-methyl-6-(4-methylpiperazin-1-yl)-9-(tetrahydro-2H-pyran-4-yl)-9H-purine
  • CS-2878
  • 9H-Purine, 8-(2-chlorophenyl)-2-methyl-6-(4-methyl-1-piperazinyl)-9-(tetrahydro-2H-pyran-4-yl)-
  • Inhibitor,LY2828360,inhibit,LY-2828360,LY 2828360,Cannabinoid Receptor
  • LY2828360, 10 mM in DMSO
CAS:
1231220-79-3
MF:
C22H27ClN6O
MW:
426.94
Mol File:
1231220-79-3.mol
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LY2828360 Chemical Properties

Boiling point:
541.8±60.0 °C(Predicted)
Density 
1.40±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
Chloroform: 30 mg/ml
form 
A crystalline solid
pka
7.15±0.10(Predicted)
color 
White to off-white
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LY2828360 Usage And Synthesis

Uses

LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.

Biological Activity

LY2828360 is a potent and selective slowly acting G protein-biased CB2 cannabinoid agonist th at inhibits cAMP accumulation and activates ERK1/2 signaling while failing to recruit arrestin. LY2828360 suppress chemotherapy-induced neuropathic pain created by paclitaxel without producing tolerance in mice.

in vivo

In WT mice, acute systemic administration of LY2828360 suppresses paclitaxel-induced mechanical and cold allodynia in a dose-dependent manner. LY2828360 produces time-dependent suppressions of paclitaxel-evoked mechanical and cold hypersensitivities and suppression of allodynia is maintained for at least 4.5 h post-injection relative to drug pre-injection levels. At 24 h post-injection, paclitaxel-induced mechanical allodynia has returned to drug pre-injection levels of hypersensitivity. Residual suppression of cold allodynia was absent by 72 h post LY2828360 treatment. Previously chronic administration of LY2828360 blocks the development of tolerance to the antiallodynic effects of morphine in WT but not in CB2KO mice. Chronic LY2828360 treatment suppresses paclitaxel-induced mechanical and cold allodynia in WT mice but not in CB2KO mice previously render tolerant to morphine[1].

References

[1] Lin X, et al. Slowly Signaling G Protein-Biased CB2 Cannabinoid Receptor Agonist LY2828360 Suppresses Neuropathic Pain with Sustained Efficacy and Attenuates Morphine Tolerance and Dependence. Mol Pharmacol. 2018 Feb;93(2):49-62. DOI:10.1124/mol.117.109355

LY2828360Supplier

Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Email
3008007409@qq.com
Shanghai Chaolan Chemical Technology Center
Tel
021-QQ：65489617 15618227136
Email
Sales@ATKchemical.com
Fan De(Beijing) Biotechnology Co., Ltd.
Tel
15911056312
Email
liming@bio-fount.com
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