2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. Ro 25-6981

Ro 25-6981 is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 has the potential for the research of parkinson's disease (PD).

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Ro 25-6981 Maleate) that retains the same biological activity.

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

Ro 25-6981 Chemical Structure

Ro 25-6981 Chemical Structure

CAS No. : 169274-78-6

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Ro 25-6981 Related Antibodies

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Description

Ro 25-6981 is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 has the potential for the research of parkinson's disease (PD)[1][2][3].

IC50 & Target

NMDA Receptor

 

In Vivo

Ro 25-6981 (0.39-12.5 mg/kg; i.p.) induces contraversive rotations in 6-hydroxydopamine (6-OHDA)-lesioned rats without stimulating locomotion in normal rats[1].
Ro 25-6981 (1,3 mg/kg; i.p.) exhibits age- and activation-dependent anticonvulsant action at early postnatal development in rats[2].
Ro 25-6981 (800 µg; intrathecal injection) shows significant analgesic effects on incision pain in rats and effectively attenuated postoperative hyperalgesia[3].

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

Animal Model: 6-OHDA-lesioned rats[1]
Dosage: 0.39-12.5 mg/kg
Administration: I.p.
Result: Dose-dependently induced contraversive tight nose-to-tail rotations, and induced a weak ipsiversive circling response indicating a mild unspecific stimulatory action of the compound.
Animal Model: Male albino rats of Wistar strain[2]
Dosage: 1, 3 mg/kg
Administration: I.p.
Result: Caused a significant decrease of N1–P2 amplitude at higher stimulation intensities AT 3 mg/kg, and exhibited age- and activation-dependent anticonvulsant action at early postnatal development.
Molecular Weight

339.47

Formula

C22H29NO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC1=CC=C([C@H](O)[C@@H](C)CN2CCC(CC3=CC=CC=C3)CC2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (736.44 mM; Need ultrasonic; 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 2.9458 mL 14.7288 mL 29.4577 mL
5 mM 0.5892 mL 2.9458 mL 5.8915 mL
View the Complete Stock Solution Preparation Table

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.5 mg/mL (7.36 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.36 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
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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
References

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9458 mL 14.7288 mL 29.4577 mL 73.6442 mL
5 mM 0.5892 mL 2.9458 mL 5.8915 mL 14.7288 mL
10 mM 0.2946 mL 1.4729 mL 2.9458 mL 7.3644 mL
15 mM 0.1964 mL 0.9819 mL 1.9638 mL 4.9096 mL
20 mM 0.1473 mL 0.7364 mL 1.4729 mL 3.6822 mL
25 mM 0.1178 mL 0.5892 mL 1.1783 mL 2.9458 mL
30 mM 0.0982 mL 0.4910 mL 0.9819 mL 2.4548 mL
40 mM 0.0736 mL 0.3682 mL 0.7364 mL 1.8411 mL
50 mM 0.0589 mL 0.2946 mL 0.5892 mL 1.4729 mL
60 mM 0.0491 mL 0.2455 mL 0.4910 mL 1.2274 mL
80 mM 0.0368 mL 0.1841 mL 0.3682 mL 0.9206 mL
100 mM 0.0295 mL 0.1473 mL 0.2946 mL 0.7364 mL
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Ro 25-6981 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:

Ro 25-6981169274-78-6iGluRIonotropic glutamate receptorsparkinson's diseaseanticonvulsantanti-parkinsonianInhibitorinhibitorinhibit

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