ONO-8590580 |
| Katalog-Nr.GC19271 |
ONO-8590580 ist ein GABAA-α5-negativer allosterischer Modulator.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1802661-73-9
Sample solution is provided at 25 µL, 10mM.
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ONO-8590580 is a GABAA α5 negative allosteric modulator.
The effect of ONO-8590580 on the MK-801/scopolamine-induced cognitive deficit in the 8-arm radial maze test is investigated. Doses of MK-801 and scopolamine for this test are 0.075 mg/kg (i.p.) and 0.2 mg/kg (i.p.) respectively. ONO-8590580 (20 mg/kg, p.o.) significantly decreases the number of errors and total latency compared to the control. The present study in which ONO-8590580 but not donepezil significantly decreases the number of errors may suggest that ONO-8590580 could be more potent for the treatment of AD patients. The data showing that ONO-8590580 has not anxiogenic-like or proconvulsant effects are in agreement with the behavioral phenotype of α5-/- mice[1].
References:
[1]. Kawaharada S, et al. ONO-8590580, a Novel GABAAα5 Negative Allosteric Modulator Enhances Long-Term Potentiation and Improves Cognitive Deficits in Preclinical Models. J Pharmacol Exp Ther. 2018 Jul;366(1):58-65.
Animal experiment: | Rats[1]Male Sprague-Dawley rats are used. ONO-8590580 is orally administered 1 h before sacrifice. [3H]-Ro15-4513 (1.11 MBq/kg) is administered via the tail vein (1 mL/kg) 10 min before sacrifice. Rats (n=12 in each group) are given either vehicle, ONO-8590580 (20 mg/kg, p.o.), or as a positive control, the GABAA nonselective NAM FG-7142 (15 mg/kg, i.p.). After 1 h, rats are placed in the elevated plus maze for 5 min. Light intensity in the open arms is set at 20 lx. A video camera fitted with a polarizing lens is mounted above the maze, connected to a tracking and analyse system[1]. Mice[1]Mice (n=8 in each group) are intraperitoneally administered with either vehicle, ONO-8590580 (10 mg/kg), or FG-7142 (10 mg/kg). After 30 min, the mice are infused with 15 mg/mL PTZ solution (infusion rate 0.2 mL/min), and the time taken to reveal clonic seizures is measured, and from this the dose administrated is calculated[1]. |
References: [1]. Kawaharada S, et al. ONO-8590580, a Novel GABAAα5 Negative Allosteric Modulator Enhances Long-Term Potentiation and Improves Cognitive Deficits in Preclinical Models. J Pharmacol Exp Ther. 2018 Jul;366(1):58-65. | |
| Cas No. | 1802661-73-9 | SDF | |
| Canonical SMILES | CN1C=C(C2=CN=C(NC3=C(F)C(C)=C4N=CN(CC5CC5)C4=C3)C=C2)N=C1 | ||
| Formula | C21H21FN6 | M.Wt | 376.43 |
| Löslichkeit | DMSO : 62.5 mg/mL (166.03 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6565 mL | 13.2827 mL | 26.5654 mL |
| 5 mM | 0.5313 mL | 2.6565 mL | 5.3131 mL |
| 10 mM | 0.2657 mL | 1.3283 mL | 2.6565 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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