2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. 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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ONO-9517601

ONO-9517601 Chemical Structure

CAS No. : 2640753-22-4

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ONO-9517601 Related Antibodies

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Description

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[1].

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.

ONO-9517601 Related Antibodies
In Vivo

ONO-9517601 (0.1-30 mg/kg, p.o., 3.5 h pre-MK-801) improves recognition memory in MK-801 challenge rats[1].
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.
Molecular Weight

461.94

Formula

C25H24ClN5O2
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ONO-9517601 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ONO-95176012640753-22-4VU6022856ONO9517601ONO 9517601VU 6022856VU-6022856Potassium ChannelKcsApreclinical research toolsrobust efficacyion channel selectivityMK-801 challenge rat NOR paradigmKP family of potassium ion channelsCNS penetrantselective TREK inhibitionOPTimizationpotencyPK profilesTREK inhibitorsInhibitorinhibitorinhibit

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