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.
For research use only. We do not sell to patients.
- CAS No.: 2640753-27-9
- Formula: C25H22ClF2N5O2
- Molecular Weight:497.92
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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 0.11 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. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | T1/2 | CLplasma | Vss | Cmax | F |
|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 5.5 h | 6.1 mL/min/kg | 2.7 L/kg | / | / |
| Rat[1] | 1 mg/kg | p.o. | / | / | / | 162 ng/mL | 57 % |
| Dog[1] | 0.5 mg/kg | i.v. | 76 h | 1.5 mL/min/kg | 7.1 L/kg | / | / |
| Dog[1] | 1 mg/kg | p.o. | / | / | / | 263 ng/mL | 100 % |
| Cynomolgus Monkey[1] | 1 mg/kg | i.v. | 9.3 h | 6.5 mL/min/kg | 4.4 L/kg | / | / |
| Cynomolgus Monkey[1] | 1 mg/kg | p.o. | / | / | / | 260 L/kg | 89 % |
In Vivo
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.
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Animal Model:Male rats[1]
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Dosage:0.03, 0.1, 0.3, 1, and 3 mg/kg
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Administration:P.O., 3.5 h pre-MK-801
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Result:Improved recognition memory in male rats after MK-801 challenge. Significantly reversed the MK-801 deficit at 1 mg/kg。
Chemical Information
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CAS No. 2640753-27-9
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Molecular Weight 497.92
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Formula C25H22ClF2N5O2
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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
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Synonyms
VU6024391
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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-7927846 Related Classifications
HY-179005 Related Classifications
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Keywords
- ONO-7927846
- 2640753-27-9
- VU6024391
- ONO7927846
- ONO 7927846
- VU 6024391
- VU-6024391
- Potassium Channel
- preclinical research tools
- robust efficacy
- -acyl piperidine pyrazoles
- ion channel selectivity
- MK-801 challenge rat NOR paradigm
- OPTIMIZATION
- CNS penetrant
- KP family of potassium ion channels
- potency
- PK profiles
- TREK inhibitors
- Inhibitor
- inhibitor
- inhibit