J-115814
J-115814 is a potent and selective neuropeptide Y1 antagonist with Ki values of 1.4, 1.8, 1.9, >10000, 620, 6000, >10000 nM for hY1, rY1, mY1, hY2, hY4, hY5, mY6, respectively. J-115814 inhibits feeding behaviors.
For research use only. We do not sell to patients.
- CAS No.: 329716-61-2
- Formula: C29H38ClN5O3S
- Molecular Weight:572.16
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Neuropeptide Y Receptor Isoforms
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Biological Activity
|
hY1 receptor 1.4 nM (Ki) |
rNPY Y1 receptor 1.8 nM (Ki) |
mY1 1.9 nM (Ki) |
hY4 receptor 620 nM (Ki) |
hY5 receptor 6000 nM (Ki) |
human Y2 receptor >10000 nM (Ki) |
mY6 >10000 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1.4 nM
Compound: 1
|
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
Displacement of [125I]PYY from human recombinant NPY Y1 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding by scintillation counting
|
[PMID: 19487123] |
| HEK293 | IC50 |
0.036 μM
Compound: 1
|
Displacement of [35S]MK499 from human ERG channel in HEK293 cells
Displacement of [35S]MK499 from human ERG channel in HEK293 cells
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[PMID: 19487123] |
J-115814 (3, 10, 30 mg/kg; i.p.) shows anorexigenic effect in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:db/db and lean C57BL6 mice[1]
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Dosage:3, 10, 30 mg/kg
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Administration:I.p.
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Result:Decreasesd nocturnal food intake in a dose-dependent manner.
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Animal Model:SD rats[1]
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Dosage:0.3, 1, 3, 10 mg/kg
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Administration:I.v.; 1 h before ICV NPY
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Result:Inhibited NPY-induced feeding with significant responses at 3 and 10 mg/kg.
Chemical Information
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CAS No. 329716-61-2
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Molecular Weight 572.16
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Formula C29H38ClN5O3S
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SMILES
CC1=C(SC(CCC2=CC(N3CCOCC3)=CC(NC(C)C4=CC(NC(OC(C)C)=O)=CC(Cl)=C4)=N2)=N1)CC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)