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.
For research use only. We do not sell to patients.
- CAS No.: 2640753-22-4
- Formula: C25H24ClN5O2
- Molecular Weight:461.94
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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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Molecular Weight 461.94
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Formula 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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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.
Protocols
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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.
Purity & Documentation
References
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