2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. ONO-7927846

ONO-7927846 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.11 μM, TREK-2 IC50= 0.29 μM). ONO-7927846 displays robust efficacy in an MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm. ONO-7927846 can be used for research on neurological and cognitive disorders.

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ONO-7927846

ONO-7927846 Chemical Structure

CAS No. : 2640753-27-9

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ONO-7927846 Related Antibodies

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Description

ONO-7927846 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.11 μM, TREK-2 IC50= 0.29 μM). ONO-7927846 displays robust efficacy in an MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm. ONO-7927846 can be used for research on neurological and cognitive disorders[1].

IC50 & Target[1]

TREK-1

0.11 μM (IC50)

TREK-2

0.29 μM (IC50)

In Vitro

ONO-7927846 (10 μM) displays >50% inhibition against adenosine A3 (91%) and sodium channel site 2 (56%); shows minimal activity against Cav1.2, HCN4, Kir2.1, Kv1.5, Kv4.3, Kir2.2, and Nav1.5; and functionally inhibits hERG with an IC50/sub> of 4.3 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ONO-7927846 Related Antibodies
In Vivo

ONO-7927846 (0.03-3 mg/kg; p.o.; 3.5 h pre-MK-801) displays robust efficacy in an MK-801 challenge rat novel object recognition (NOR) paradigm[1].
ONO-7927846 (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: 0.03, 0.1, 0.3, 1, and 3 mg/kg
Administration: P.O., 3.5 h pre-MK-801
Result: Improved recognition memory in male rats after MK-801 challenge. Significantly reversed the MK-801 deficit at 1 mg/kg。
Molecular Weight

497.92

Formula

C25H22ClF2N5O2
CAS No.
SMILES

CC1=C(N=CC(C#CC2=CC=C(C=C2)F)=C1)NC(C3=C(C=NN3[C@H]4[C@@H](CN(CC4)C(C)=O)F)Cl)=O
Shipping

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-7927846 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-79278462640753-27-9VU6024391ONO7927846ONO 7927846VU 6024391VU-6024391Potassium ChannelKcsApreclinical research toolsrobust efficacy-acyl piperidine pyrazolesion channel selectivityMK-801 challenge rat NOR paradigmOPTIMIZATION CNS penetrantKP family of potassium ion channelspotencyPK profilesTREK inhibitorsInhibitorinhibitorinhibit

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