1. GPCR/G Protein
  2. Cannabinoid Receptor

LY2828360 

目录号: HY-16642A
产品使用指南

LY2828360 是一个作用缓慢但很有效的 G 蛋白偏倚的大麻素受体 2 (CB2) 激动剂,能够抑制 cAMP 的积累并激活 ERK1/2 通路。

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LY2828360 Chemical Structure

LY2828360 Chemical Structure

CAS No. : 1231220-79-3

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥2310 In-stock
5 mg ¥2100 In-stock
10 mg ¥3400 In-stock
25 mg ¥6800 In-stock
50 mg ¥9500 In-stock
100 mg ¥15000 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

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

IC50 & Target

CB2[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 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].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : 20.83 mg/mL (48.79 mM; Need ultrasonic)

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.87 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.87 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.87 mM); Clear solution

References
Molecular Weight

426.94

Formula

C₂₂H₂₇ClN₆O

CAS No.

1231220-79-3

SMILES

CN1CCN(C2=C3N=C(C4=CC=CC=C4Cl)N(C5CCOCC5)C3=NC(C)=N2)CC1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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产品名称:
LY2828360
目录号:
HY-16642A
需求量:

LY2828360

Cat. No.: HY-16642A