AGMO-IN-1
AGMO-IN-1 is an alkylglycerol monooxygenase (AGMO) inhibitor. AGMO-IN-1 competitively binds with BH4 at the cofactor-binding site of BH4-dependent AGMO, inhibiting AGMO activity (rat IC50 = 26-100 µM); AGMO-IN-1 shows weaker inhibitory activity against PAH and NOS than against AGMO. AGMO-IN-1 inhibits preadipocyte differentiation, reduces lipid droplet accumulation in adipocytes and hepatocytes, blocks IL-4-induced M2-like polarization of macrophages, and slows cell cycle progression during the mitotic clonal expansion phase, making it useful for research related to nonalcoholic hepatic steatosis.
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- CAS No.: 91901-11-0
- Formule: C10H17N5O
- Masse moléculaire:223.27
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[1]|
AGMO 26-100 μM (IC50, rat) |
PAH 360-430 μM (IC50, rat) |
NOS 1.9-5.3 mM (IC50) |
In Vitro
AGMO-IN-1 (100-300 µM; 24 h) reduces FFA-induced lipid droplet accumulation in HepG2 hepatocytes but does not prevent FFA-induced loss of viability[1].
AGMO-IN-1 (300 µM; differentiation days 0-7) is characterized during 3T3-L1 adipocyte differentiation, and Pref-1/FABP4 marker expression and morphology are monitored until day 7[1].
AGMO-IN-1 (300 µM; day 7 of differentiation) produces BODIPY-488-positive lipid droplets in 3T3-L1 adipocytes[1].
AGMO-IN-1 (300 µM; days 5-7 of differentiation, combined time points) is associated with changes in Oil Red O lipid titer quantification in differentiating 3T3-L1 adipocytes[1].
AGMO-IN-1 (0.1-1000 µM; 24 h) reduces the viability/proliferation of low-density 3T3-L1 cells with an IC50 of 300-400 µM, but has no effect at high culture density[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:3T3-L1 mouse preadipocytes
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Concentration:0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 µM
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Incubation Time:24 h
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Result:No growth-inhibitory or cytotoxic effect occurred in high-density 3T3-L1 cultures.
In low-density cultures, viability and proliferation were reduced with half-maximum effect at 300-400 µM.
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Cell Line:3T3-L1 mouse preadipocytes
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Concentration:300 µM and 1 mM
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Incubation Time:48 h pretreatment from 72 h; continuous exposure through day 6; washout day 7-10; endpoint day 10
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Result:At 1 mM, 3T3-L1 proliferation and differentiation were almost completely suppressed from day 3-10.
Washout at day 7 restored proliferation, but cells did not accumulate adipocyte lipid droplets by day 10, whereas vehicle-treated cultures had abundant lipid droplets.
At 300 µM, the Pref-1-to-FABP4 switch and Oil-Red O staining were reduced, with some cells appearing hypertrophic.
Cells did not increase AGMO, eNOS, PPARγ, or CEBPα expression during differentiation.
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Cell Line:3T3-L1 mouse preadipocytes
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Concentration:300 µM
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Incubation Time:cell-cycle analysis at baseline, 1 d, and 3 d after IDI; cyclin mRNA at days 0, 1, 3, and 7 after IDI
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Result:At 1 d after IDI, more cells were in S phase; at 3 d, more cells were in G2 phase.
G1 cells were reduced, and sub-G1 cells increased.
Cyclin D (CCND2/CCND3) mRNA was increased and cyclin A2 (CCNA2) mRNA was reduced.
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Cell Line:HepG2 human hepatocytes
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Concentration:0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 µM (viability assay); 100 or 300 µM (FFA experiments)
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Incubation Time:24 h incubations; FFA exposure up to 24 h
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Result:No effect on HepG2 viability occurred up to high concentrations.
The FFA-evoked drop in HepG2 viability/proliferation was not prevented, but FFA-evoked lipid droplet accumulation by Oil-Red O was reduced at 24 h.
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Cell Line:RAW264.7 macrophages (shLUC, shAGMO, +huAGMO)
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Concentration:0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 µM
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Incubation Time:24 h
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Result:No additional deleterious effect on viability occurred in shAGMO RAW264.7 cells.
SRB and WST readouts were moderately reduced in shLUC and +huAGMO cells only at high concentrations.
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Cell Line:+huAGMO RAW264.7 macrophages
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Concentration:100 µM
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Incubation Time:48 h
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Result:IL-4-induced M2 markers Tgm2, Arg1, MRC1/CD206, and Alox15 were reduced.
LPS/IFNγ-induced M1 markers IL23a, IL6, and TNFα were increased.
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Cell Line:3T3-L1 pre/adipocytes
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Concentration:300 µM
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Incubation Time:d0, d1, d3, and d7 of differentiation
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Result:Time-course imaging showed morphology and Pref-1/FABP4 immunofluorescence at d0, d1, d3, and d7.
Pref-1 and FABP4 signals were displayed across the differentiation time course.
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Cell Line:3T3-L1 adipocytes
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Concentration:300 µM
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Incubation Time:day 7 of differentiation
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Result:BODIPY-488 staining showed lipid droplets in 3T3-L1 cells at day 7.
DAPI-stained nuclei were visible.
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Cell Line:3T3-L1 adipocytes
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Concentration:300 µM
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Incubation Time:days 5 and 7 of differentiation, pooled time points
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Result:Oil Red O lipid droplet quantification at pooled days 5 and 7 showed a difference versus vehicle.
Chemical Information
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CAS No. 91901-11-0
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Masse moléculaire 223.27
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Formule C10H17N5O
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SMILES
O=C1N=C(N(C)C)NC2=C1NC(C)C(C)N2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)