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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- CAS No.: 2640753-27-9
- 화학식: C25H22ClF2N5O2
- 분자량:497.92
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보관:
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
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TREK-1 0.11 μM (IC50) |
TREK-2 0.29 μM (IC50) |
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.
| 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 % |
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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분자량 497.92
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ONO-7927846 Related Classifications
HY-179005 Related Classifications
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- 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