1. Neuronal Signaling Metabolic Enzyme/Protease Apoptosis
  2. Imidazoline Receptor Mitochondrial Metabolism Caspase Lactate Dehydrogenase
  3. AGN 192403

AGN 192403 (BRD4780) is a potent and selective imidazoline-1 receptor antagonist with a Ki value of 42 nM. AGN 192403 is also a TMED9 inhibitor. AGN 192403 shows protective effects on oxidative cytotoxicity and mitochondrial inhibitor-induced cytotoxicity in astrocytes. AGN 192403 mitigates the proliferation and migration of differentiated glioma tumor cells. AGN 192403 can be used for glioma tumor and neurological diseases research.

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AGN 192403

AGN 192403 Chemical Structure

CAS No. : 175521-95-6

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Description

AGN 192403 (BRD4780) is a potent and selective imidazoline-1 receptor antagonist with a Ki value of 42 nM. AGN 192403 is also a TMED9 inhibitor. AGN 192403 shows protective effects on oxidative cytotoxicity and mitochondrial inhibitor-induced cytotoxicity in astrocytes. AGN 192403 mitigates the proliferation and migration of differentiated glioma tumor cells. AGN 192403 can be used for glioma tumor and neurological diseases research[1][2].

IC50 & Target[1]

Caspase-9

 

imidazoline-1 receptor

42 nM (Ki)

In Vitro

AGN 192403 (10-100 μM, 24 h) inhibits the former lysosomal destabilization and the subsequent decrease in mitochondrial potential in astrocytes exposed to Naphthazarin (HY-N7526)[1].
AGN 192403 (10-100 μM, 24 h) inhibits the Antimycin A- and Rotenone (HY-B1756)-induced decrease in mitochondrial potential, cytochrome c release, caspase-9 activation, and eventually LDH release in astrocytes[1].
AGN 192403 (4-25 μM, 14 days) exerts a remarkable inhibitory effect on glioma stem cells (GSC)s self-renewal, demonstrating almost complete inhibition of self-renewal at the highest concentration applied[2].
AGN 192403 (0-25 μM, 18-48 h) targets TMED9, reduces the stemness, reduces GSC migration, and inhibits GSC tumorigenic functions[2].
AGN 192403 (4-25 μM, 0-8 days) induces cell death in a dose dependent manner in patient-derived GSCs[2].
AGN 192403 (4-25 μM, 48 h-8 days) inhibits TMED9 and exerts anti-tumor effects in diffuse intrinsic pontine glioma (DIPG) cells[2].

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

Western Blot Analysis[2]

Cell Line: patient-derived GSCs
Concentration: 0, 4, 10, 25 μM
Incubation Time: 48 h
Result: Decreased TMED9 expression in a dose-dependent manner in three different patient-derived GSCs.

RT-PCR[2]

Cell Line: GSCs
Concentration: 10, 25 μM
Incubation Time: 48 h
Result: Showed a marked and dose dependent reduction in SOX2 expression.
Markedly reduced YKL40 expression.

Cell Migration Assay [2]

Cell Line: GSCs
Concentration: 10, 25 μM
Incubation Time: 18-20 h
Result: Dose-dependently reduced GSC migration.

Cell Viability Assay[2]

Cell Line: GSCs
Concentration: 4, 10, 25 μM
Incubation Time: 0, 1, 2, 3, 4, 5, 6, 7, 8 days
Result: Resulted in a dose-dependent induction of cell death, at multiple points over the course of one week.
In Vivo

AGN 192403 (3000 μg/kg, i.v., single dose pretreat) can bloack imidazoline-1 receptor without modifying the baseline values of heart rate and blood pressure in rats[3].

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

Molecular Weight

153.26

Formula

C10H19N

CAS No.
SMILES

CC([C@H]1[C@@]2([H])C[C@@](CC2)([H])[C@@H]1N)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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AGN 192403
Cat. No.:
HY-101374
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