1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor

ONO-8590580 

目录号: HY-112788 纯度: 99.85%
产品使用指南

ONO-8590580 是 GABAA α5 的负变构调节剂.

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ONO-8590580 Chemical Structure

ONO-8590580 Chemical Structure

CAS No. : 1802661-73-9

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Description

ONO-8590580 is a GABAA α5 negative allosteric modulator.

IC50 & Target

GABAA α5[1].

In Vivo

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].

Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (166.03 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.53 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.53 mM); Clear solution

References
Animal Administration
[1]

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].

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

References
Molecular Weight

376.43

Formula

C₂₁H₂₁FN₆

CAS No.

1802661-73-9

SMILES

CN1C=C(C2=CN=C(NC3=C(F)C(C)=C4N=CN(CC5CC5)C4=C3)C=C2)N=C1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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C1   V1   C2   V2

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产品名称:
ONO-8590580
目录号:
HY-112788
需求量:

ONO-8590580

Cat. No.: HY-112788