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.
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- CAS No.: 2640753-22-4
- Formule: C25H24ClN5O2
- Masse moléculaire:461.94
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
TREK-1 0.067 μM (IC50) |
TREK-2 0.23 μM (IC50) |
In Vitro
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 | / | / |
In Vivo
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.
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Animal Model:Male rats[1]
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Dosage:0.1, 0.3, 1, 3, 10, 30 mg/kg
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Administration:p.o., 3.5 h pre-MK-801
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Result:Significantly reversed the MK-801 deficit at 1, and 3 mg/kg. Improved recognition memory in rats.
Chemical Information
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CAS No. 2640753-22-4
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Masse moléculaire 461.94
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Formule C25H24ClN5O2
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SMILES
CC1=C(N=CC(C#CC2=CC=CC=C2)=C1)NC(C3=C(C=NN3C4CCN(CC4)C(C)=O)Cl)=O
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Synonyms
VU6022856
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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.
Protocole
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ONO-9517601 Related Classifications
HY-179004 Related Classifications
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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