ONO-9517601
ONO-9517601 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.067 μM, TREK-2 IC50= 0.23 μM). ONO-9517601 displays robust efficacy in an MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm. ONO-9517601 can be used for research on neurological and cognitive disorders.
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: 2640753-22-4
- 分子式: C25H24ClN5O2
- 分子量:461.94
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
TREK-1 0.067 μM (IC50) |
TREK-2 0.23 μM (IC50) |
体外実験
ONO-9517601 (10 μM) inhibits adenosine A3 (98%) and DAT (78%), exhibits minimal activity against Cav1.2, HCN4, Kir2.1, Kv1.5, Kv4.3, KCNQ1/E1, and Nav1.5, shows no significant effect on TASK-1, TASK-2, THIK-1, and TRESK, and blocks hERG with an IC50 of 6.7 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | Vss | T1/2 | CLplasma | Cmax | F |
|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 2.2 L/kg | 1.0 h | 30.0 mL/min/kg | / | / |
| Rat[1] | 1 mg/kg | p.o. | / | / | / | 80 ng/mL | 40 % |
| Cynomolgus Monkey[1] | 1 mg/kg | p.o. | / | / | / | 152 ng/mL | 34 % |
| Cynomolgus Monkey[1] | 1 mg/kg | i.v. | 2.1 L/kg | 3.3 h | 13.3 mL/min/kg | / | / |
| Dog[1] | 1 mg/kg | p.o. | / | / | / | 315 ng/mL | 97 % |
| Dog[1] | 1 mg/kg | i.v. | 5.9 L/kg | 56 h | 1.9 mL/min/kg | / | / |
体内実験
ONO-9517601 (56.6 mg/kg, p.o., single dose) results in no significant neurobehavioral alterations in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male rats[1]
-
Dosage:0.1, 0.3, 1, 3, 10, 30 mg/kg
-
Administration:p.o., 3.5 h pre-MK-801
-
Result:Significantly reversed the MK-801 deficit at 1, and 3 mg/kg. Improved recognition memory in rats.
化学情報
-
CAS 番号 2640753-22-4
-
分子量 461.94
-
分子式 C25H24ClN5O2
-
SMILES
CC1=C(N=CC(C#CC2=CC=CC=C2)=C1)NC(C3=C(C=NN3C4CCN(CC4)C(C)=O)Cl)=O
-
別名
VU6022856
-
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.
プロトコル
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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)
ONO-9517601 関連分類
HY-179004 関連分類
Powered by Bioz
Keywords
- ONO-9517601
- 2640753-22-4
- VU6022856
- ONO9517601
- ONO 9517601
- VU 6022856
- VU-6022856
- Potassium Channel
- preclinical research tools
- robust efficacy
- ion channel selectivity
- MK-801 challenge rat NOR paradigm
- KP family of potassium ion channels
- CNS penetrant
- selective TREK inhibition
- OPTimization
- potency
- PK profiles
- TREK inhibitors
- Inhibitor
- inhibitor
- inhibit