PIPE-3297
PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC50 of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity.
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。
- 分子式: C23H30N2O
- 分子量:350.50
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Opioid 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
|
κ Opioid Receptor/KOR 1.1 nM (EC50) |
体外実験
PIPE-3297 induces myelination and causes oligodendrocyte progenitor cells (OPCs) differentiation into oligodendrocytes (OLs)[1].
PIPE-3297 exhibits cardiotoxity with 72% hERG inhibition (3 μM) and unstability in liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:OPC
-
Concentration:0.5-1 μM
-
Incubation Time:72 h
-
Result:Increased levels of MBPs
体内実験
PIPE-3297 (30 mg/kg, s.c., single dosage) induces KOR-dependent OPC differentiation into mature OLs in C57BL/6 mice[1].
PIPE-3297 (3 and 30 mg/kg, s.c., daily for 23 days) ameliorates the autoimmune encephalomyelitis (EAE) induced by myelin oligodendrocyte glycoprotein (MOG) in C57BL/6 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:MOG induced EAE in C57BL/6 mice[1]
-
Dosage:3 and 30 mg/kg
-
Administration:s.c., daily for 23 days
-
Result:Ameliorated the EAE.
-
Animal Model:C57BL/6 mice[1]
-
Dosage:3 and 30 mg/kg
-
Administration:s.c., single dose
-
Result:Increased levels of KOR and mature OLs, maintained the locomotion ability.
化学情報
-
分子量 350.50
-
分子式 C23H30N2O
-
SMILES
OC1=CC=CC(CCN(C2CN(C2)CC3=CC=CC=C3)CC4CCC4)=C1
-
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)