1. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  2. Nuclear Hormone Receptor 4A/NR4A RAR/RXR
  3. XCT0135908

XCT0135908 (XCT) is a selective Nurr1-RXRα activator with an EC50 value of 0.3 μM in human dopaminergic SH-SY5Y cells. XCT0135908 protects dopaminergic cells against the Parkinson’s disease-related toxin MPP+. XCT0135908 can be used for the research of Parkinson’s disease.

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XCT0135908

XCT0135908 Chemical Structure

CAS No. : 300837-31-4

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Description

XCT0135908 (XCT) is a selective Nurr1-RXRα activator with an EC50 value of 0.3 μM in human dopaminergic SH-SY5Y cells. XCT0135908 protects dopaminergic cells against the Parkinson’s disease-related toxin MPP+. XCT0135908 can be used for the research of Parkinson’s disease[1].

In Vitro

XCT0135908 (Compound 7a) (0.5-12.5 μM; overnight) activates the Nurr1-RXRα heterodimer in human dopaminergic SH-SY5Y cells with an EC50 of 0.3 μM[1].
XCT0135908 (0.5-12.5 μM; 12 h) selectively activates Nurr1-RXRα and Nur77-RXRα heterodimers (but not other RXRα heterodimers or homodimers) in human dopaminergic SH-SY5Y cells, with greater activation of Nur77GAL4-RXRαVP16 than Nurr1GAL4-RXRαVP16[1].
XCT0135908 (12.5-50 μM) protects mouse Neuro-2a neuroblast cells from MPP+-induced toxicity at concentrations of 12.5 μM and 50 μM, with no observed toxicity at 50 μM[1].
XCT0135908 (0.5-12.5 μM; 24 h) induces a moderate concentration-dependent increase in SREBP-1c expression in human HepG2 hepatic cells, with a maximal ~5-fold increase at 12.5 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR[1]

Cell Line: human HepG2 hepatic cells
Concentration: 0.5 μM; 12.5 μM
Incubation Time: 24 h
Result: Triggered a concentration-dependent increase in SREBP-1c expression.
Induced a maximal increase of ~5-fold over controls.
Molecular Weight

345.40

Formula

C21H19N3O2

CAS No.
SMILES

O=C(O)C1=CC=C(C=C1)NC2=NC(=NC(=C2CC=C)C)C=3C=CC=CC3

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Product Name:
XCT0135908
Cat. No.:
HY-119612
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