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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 329716-61-2
- 分子式: C29H38ClN5O3S
- 分子量:572.16
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Neuropeptide Y Receptor アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
[1]|
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) |
Cellular Effect
|
Cell Line
|
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
|
[PMID: 19487123] |
体内実験
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.
-
Animal Model:db/db and lean C57BL6 mice[1]
-
Dosage:3, 10, 30 mg/kg
-
Administration:I.p.
-
Result:Decreasesd nocturnal food intake in a dose-dependent manner.
-
Animal Model:SD rats[1]
-
Dosage:0.3, 1, 3, 10 mg/kg
-
Administration:I.v.; 1 h before ICV NPY
-
Result:Inhibited NPY-induced feeding with significant responses at 3 and 10 mg/kg.
化学情報
-
CAS 番号 329716-61-2
-
分子量 572.16
-
分子式 C29H38ClN5O3S
-
SMILES
CC1=C(SC(CCC2=CC(N3CCOCC3)=CC(NC(C)C4=CC(NC(OC(C)C)=O)=CC(Cl)=C4)=N2)=N1)CC
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)