[CAS NO. 1231220-79-3] LY2828360
PRODUCTS SPECIFICATIONS [1231220-79-3]
DESCRIPTION [1231220-79-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 426.94 |
| Molecular Formula | C22H27ClN6O |
| SMILES | CN1CCN(C2=C3N=C(C4=CC=CC=C4Cl)N(C5CCOCC5)C3=NC(C)=N2)CC1 |
Summary
LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB 2 ) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
IC50 & Target
CB 2 [1] .
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 CB 2 KO mice. Chronic LY2828360 treatment suppresses paclitaxel-induced mechanical and cold allodynia in WT mice but not in CB 2 KO mice previously render tolerant to morphine [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01319929 | Eli Lilly and Company |
Osteoarthritis, Knee
|
March 2011 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 20.83 mg/mL ( 48.79 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3422 mL | 11.7112 mL | 23.4225 mL |
| 5 mM | 0.4684 mL | 2.3422 mL | 4.6845 mL |
| 10 mM | 0.2342 mL | 1.1711 mL | 2.3422 mL |
