Dendrogenin A

一种选择性的LXR调节剂和ChEH抑制剂。

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库存: 现货

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1mg

￥525.00

420.00

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5mg

￥1700.00

1360.00

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10mg

￥3137.00

2510.00

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货号: ajcf22738
CAS: 1191043-85-2
别名: DDA
分子式: C32H55N3O2
分子量: 513.8
纯度: ＞98%
溶解度: DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml
储存: Store at -20°C
库存: 现货

Background

Dendrogenin A (DDA) is a selective liver X receptor (LXR) modulator (SLiM), an inhibitor of cholesterol epoxide drolase (ChEH; K_i = 120 nM), and an active metabolite of cholesterol.^1,2 It is formed from 5,6α-epoxy cholesterol via conjugation with histamine by DDA synthase.^2,1,3 DDA is found in non-cancerous human mammary epithelial cells and epithelial melanocytes but not in a variety of breast carcinoma or melanoma cells and only at low levels in isolated human breast tumor tissue.² It inhibits 22(R)-droxy cholesterol-induced activation of LXRβ and LXRα in a reporter assay (IC₅₀s = 76 and 362 nM, respectively) but is also a partial agonist of LXRs, increasing protein levels of Nur77, NOR-1, LC3-I, and LC3-II in B16/F10 murine melanoma cells.⁴ It is selective for modulation of LXRα and LXRβ over the pregnane X receptor (PXR), aryl drocarbon receptor (AhR), vitamin D receptor (VDR), retinoid X receptor γ (RXRγ), retinoic acid receptor α (RARα), peroxisome proliferator-activated receptor α (PPARα), PPARγ, glucocorticoid receptor, androgen receptor, estrogen receptor α (ERα), and ERβ at 2.5 μM. It also increases protein levels of LC3-II in B16/F10 and SK-MEL-28 cancer cells when used at concentrations of 2.5 and 5 μM and induces autophagic cell death in the same cell types at 2.5 μM. DDA (0.37 μg/kg) reduces tumor growth in a B16/F10 murine model of melanoma and a TS/A murine mammary cancer model and induces cancer cell differentiation in vitro and in vivo.²

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Dendrogenin A

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Background

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