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首页-小分子抑制剂&激动剂-GPCR-Cannabinoid Receptor-VCE-004.3
VCE-004.3

Chemical Structure : VCE-004.3

CAS No.: 1818428-14-6

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VCE-004.3 (VCE004.3)

货号: PC-35536Not For Human Use, Lab Use Only.

VCE-004.3 (VCE004.3) is a novel semi-synthetic cannabidiol derivative behaving as a dual PPARγ/CB2 agonist and CB1 receptor modulator, binds and activates PPARγ (IC50=3.5 uM) and CB2 receptors (pKi=6.69) and antagonizes CB1 receptor (pKi=5.61).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    VCE-004.3 (VCE004.3) is a novel semi-synthetic cannabidiol derivative behaving as a dual PPARγ/CB2 agonist and CB1 receptor modulator, binds and activates PPARγ (IC50=3.5 uM) and CB2 receptors (pKi=6.69) and antagonizes CB1 receptor (pKi=5.61).
    VCE-004.3 binds to an alternative site at the PPARγ ligand-binding pocket (LBP).
    VCE-004.3 inhibits collagen gene transcription and synthesis and prevents TGFβ-induced fibroblast migration and differentiation to myofibroblasts.
    VCE-004.3 prevents skin fibrosis, myofibroblast differentiation and ERK1/2 phosphorylation in bleomycin-induced skin fibrosis.
    VCE-004.3 reduces mast cell degranulation, macrophage activation, T lymphocytes infiltration, and the expression of inflammatory and profibrotic factors.

    物理化学性质&存储条件

    分子量 413.602
    分子式 C26H39NO3
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    (1'R,6'R)-6-hydroxy-3'-methyl-4-pentyl-3-(pentylamino)-6'-(prop-1-en-2-yl)-[1,1'-bi(cyclohexane)]-2',3,6-triene-2,5-dione

    参考文献

    1. Del Rio C, et al. Br J Pharmacol. 2018 Jul 22. doi: 10.1111/bph.14450.

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