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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-RAR/RXR-IRX4204
IRX4204

Chemical Structure : IRX4204

CAS No.: 220619-73-8

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IRX4204 (AGN194204, IRX-4204, AGN-194204)

货号: PC-20775Not For Human Use, Lab Use Only.

IRX4204 (AGN194204) is a potent, specific and brain penetrable pan-RXR agonist, fully activates all three RXRs (α, β and γ) at 1 nM, activates nuclear receptor Nurr1 downstream signaling.

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

    生物&药学活性

    IRX4204 (AGN194204) is a potent, specific and brain penetrable pan-RXR agonist, fully activates all three RXRs (α, β and γ) at 1 nM, activates nuclear receptor Nurr1 downstream signaling.
    IRX4204 is thousand times more potent for RXR than retinoic acid receptors (RARα, β and γ), does not activate the RXR heterodimers of farnesoid X receptor (FXR), liver X receptors (LXR) α and β, or peroxisome proliferator-activated receptor PPARγ.
    IRX4204 potently activated reporter gene transcription in a RXR dependent manner (EC50 <1 nM), IRX4204 is an effective activator of RXR/Nurr1 heterodimers.
    IRX4204 (1 nM) significantly increased the expression of dopamine transporter (DAT) and dopa-decarboxylase (DDC) in VMB neurons, which could be abolished by RXR antagonist HX531.
    IRX4204 is bioactive in the brains following oral administration and activates Nurr1 downstream genes in the substantia nigra (SN).
    IRX4204 (10mg/kg/day, oral) improves motor asymmetry and dopamine neuron loss in a rat model of PD.

    物理化学性质&存储条件

    分子量 352.52
    分子式 C24H32O2
    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

    (2E,4E)-3-methyl-5-((1S,2S)-2-methyl-2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopropyl)penta-2,4-dienoic acid

    参考文献

    1. Jun Wang, et al. Oncotarget. 2016 Feb 16;7(7):7469-79.

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