2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. ONO-8590580

ONO-8590580 is a GABAA α5 negative allosteric modulator.

For research use only. We do not sell to patients.

ONO-8590580 Chemical Structure

ONO-8590580 Chemical Structure

CAS No. : 1802661-73-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 176 In-stock
Solution
10 mM * 1 mL in DMSO USD 176 In-stock
Solid
1 mg USD 76 In-stock
5 mg USD 160 In-stock
10 mg USD 220 In-stock
25 mg USD 490 In-stock
50 mg USD 790 In-stock
100 mg USD 1250 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

ONO-8590580 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

376.43

Formula

C21H21FN6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (132.83 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.84%

COA (247 KB) HNMR (271 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6565 mL 13.2827 mL 26.5654 mL 66.4134 mL
5 mM 0.5313 mL 2.6565 mL 5.3131 mL 13.2827 mL
10 mM 0.2657 mL 1.3283 mL 2.6565 mL 6.6413 mL
15 mM 0.1771 mL 0.8855 mL 1.7710 mL 4.4276 mL
20 mM 0.1328 mL 0.6641 mL 1.3283 mL 3.3207 mL
25 mM 0.1063 mL 0.5313 mL 1.0626 mL 2.6565 mL
30 mM 0.0886 mL 0.4428 mL 0.8855 mL 2.2138 mL
40 mM 0.0664 mL 0.3321 mL 0.6641 mL 1.6603 mL
50 mM 0.0531 mL 0.2657 mL 0.5313 mL 1.3283 mL
60 mM 0.0443 mL 0.2214 mL 0.4428 mL 1.1069 mL
80 mM 0.0332 mL 0.1660 mL 0.3321 mL 0.8302 mL
100 mM 0.0266 mL 0.1328 mL 0.2657 mL 0.6641 mL
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ONO-8590580 Related Classifications

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-85905801802661-73-9ONO8590580ONO 8590580GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorInhibitorinhibitorinhibit

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