Ro 25-6981
Based on 9 publication(s) in Google Scholar
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).
For research use only. We do not sell to patients.
- Purity: 99.55%
- CAS No.: 169274-78-6
- Formula: C22H29NO2
- Molecular Weight:339.47
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Ro 25-6981
More- Cell Death Differ. 2023 Jul;30(7):1726-1741. [Abstract]
- Br J Pharmacol. 2026 Jun;183(11):2857-2873. [Abstract]
- CNS Neurosci Ther. 2023 May;29(5):1229-1242. [Abstract]
- Neurobiol Dis. 2025 Oct 15:215:107090. [Abstract]
- Neurochem Int. 2021 Feb:143:104942. [Abstract]
- Sci Rep. 2022 Oct 12;12(1):17114. [Abstract]
- Neuropharmacology. 2022 Mar 15:206:108947. [Abstract]
- Exp Brain Res. 2023 Dec;241(11-12):2735-2750. [Abstract]
- bioRxiv. 2026 Apr 23.
All iGluR Isoforms
More
Biological Activity
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NMDA Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Cortical neurone | IC50 |
0.4 μM
Compound: 11
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Neuroprotective activity in rat Cortical neuron assessed as protection from glutamate-induced neurotoxicity treated after glutamate-challenge by lactate dehydrogenase assay
Neuroprotective activity in rat Cortical neuron assessed as protection from glutamate-induced neurotoxicity treated after glutamate-challenge by lactate dehydrogenase assay
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[PMID: 23458846] |
| Oocyte | IC50 |
0.009 μM
Compound: 2, Ro-256981
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Inhibition of rat NMDA receptor NR1C/NR2B subunit expressed in Xenopus laevis oocytes after 2 days by two-electrode voltage-clamp electrophysiological assay
Inhibition of rat NMDA receptor NR1C/NR2B subunit expressed in Xenopus laevis oocytes after 2 days by two-electrode voltage-clamp electrophysiological assay
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[PMID: 23140383] |
| Oocyte | IC50 |
0.017 μM
Compound: 2, Ro-256981
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Inhibition of rat NMDA receptor NR1F/NR2B subunit expressed in Xenopus laevis oocytes after 2 days by two-electrode voltage-clamp electrophysiological assay
Inhibition of rat NMDA receptor NR1F/NR2B subunit expressed in Xenopus laevis oocytes after 2 days by two-electrode voltage-clamp electrophysiological assay
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[PMID: 23140383] |
| Oocyte | IC50 |
9 nM
Compound: 3
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Antagonist activity against rat 1A/2B subtype of N-methyl-D-aspartate (NMDA) receptor in xenopus oocytes.
Antagonist activity against rat 1A/2B subtype of N-methyl-D-aspartate (NMDA) receptor in xenopus oocytes.
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[PMID: 10386947] |
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.
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Animal Model:6-OHDA-lesioned rats[1]
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Dosage:0.39-12.5 mg/kg
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Administration:I.p.
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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.
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Animal Model:Male albino rats of Wistar strain[2]
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Dosage:1, 3 mg/kg
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Administration:I.p.
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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.
Chemical Information
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CAS No. 169274-78-6
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Appearance Solid
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Molecular Weight 339.47
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Formula C22H29NO2
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Color White to off-white
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SMILES
OC1=CC=C([C@H](O)[C@@H](C)CN2CCC(CC3=CC=CC=C3)CC2)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (9)
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Journal Impact Factor
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Most Recent
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Cell Death Differ
KCTD13-mediated ubiquitination and degradation of GluN1 regulates excitatory synaptic transmission and seizure susceptibility. [Abstract]2023 Jul;30(7):1726-1741. PMID: 37142655 -
Br J Pharmacol
GW201 mediates neuroprotection via allosteric modulation of NMDA receptor activity in the middle cerebral artery occlusion (MCAO) model. [Abstract]2026 Jun;183(11):2857-2873. PMID: 41693050 -
CNS Neurosci Ther
A decrease in NR2B expression mediated by DNA hypermethylation induces perioperative neurocognitive disorder in aged mice. [Abstract]2023 May;29(5):1229-1242. PMID: 36694341 -
Neurobiol Dis
2025 Oct 15:215:107090. PMID: 40930427 -
Neurochem Int
Astroglial adrenoreceptors modulate synaptic transmission and contextual fear memory formation in dentate gyrus. [Abstract]2021 Feb:143:104942. PMID: 33340594 -
Sci Rep
PSD-95 in the anterior cingulate cortex contributes to neuropathic pain by interdependent activation with NR2B. [Abstract]2022 Oct 12;12(1):17114. PMID: 36224339 -
Neuropharmacology
A hippocampus dependent neural circuit loop underlying the generation of auditory mismatch negativity. [Abstract]2022 Mar 15:206:108947. PMID: 35026286 -
Exp Brain Res
The NR2B-targeted intervention alleviates the neuronal injuries at the sub-acute stage of cerebral ischemia: an exploration of stage-dependent strategy against ischemic insults. [Abstract]2023 Dec;241(11-12):2735-2750. PMID: 37845379 -
Solvent & Solubility
DMSO : 100 mg/mL (294.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (2.95 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.95 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Löschmann PA, et al. Antiparkinsonian activity of Ro 25-6981, a NR2B subunit specific NMDA receptor antagonist, in animal models of Parkinson's disease. Exp Neurol. 2004 May;187(1):86-93. [Content Brief]
[2]. Szczurowska E,et al. Different action of a specific NR2B/NMDA antagonist Ro 25-6981 on cortical evoked potentials and epileptic afterdischarges in immature rats. Brain Res Bull. 2015 Feb;111:1-8. [Content Brief]
[3]. Jiang M, et al. Antinociception and prevention of hyperalgesia by intrathecal administration of Ro 25-6981, a highly selective antagonist of the 2B subunit of N-methyl-D-aspartate receptor. Pharmacol Biochem Behav. 2013 Nov;112:56-63. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| 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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