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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- No. CAS: 2640753-22-4
- Fòrmula: C25H24ClN5O2
- Peso molecular:461.94
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
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Help & FAQs
Actividad biológica
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TREK-1 0.067 μM (IC50) |
TREK-2 0.23 μM (IC50) |
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.
| 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 | / | / |
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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No. CAS 2640753-22-4
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Peso molecular 461.94
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ONO-9517601 Related Classifications
HY-179004 Related Classifications
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- 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