Ro 25-6981

Name: Ro 25-6981
Brand: MedChemExpress
SKU: HY-13993
Rating: 5.0 (6 reviews)

Cat. No.: HY-13993 Purity: 99.55%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

Ro 25-6981 Chemical Structure

CAS No. : 169274-78-6

Size	Price	Stock	Quantity
5 mg	USD 96	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 138	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Ro 25-6981:

Ro 25-6981 Maleate In-stock
Ro 25-6981 hydrochloride Get quote

6 Publications Citing Use of MCE Ro 25-6981

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AMPA Receptor NMDA Receptor Kainate Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

NMDA Receptor

Cellular Effect

Cell Line	Type	Value	Description	References
Cortical neurone	IC₅₀	0.4 μM Compound: 11	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	[PMID: 23458846]
Oocyte	IC₅₀	0.009 μM Compound: 2, Ro-256981	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	[PMID: 23140383]
Oocyte	IC₅₀	0.017 μM Compound: 2, Ro-256981	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	[PMID: 23140383]

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.

169274-78-6

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

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

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
10 mM	0.2946 mL	1.4729 mL	2.9458 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, 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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.36 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.55%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (244 KB) HNMR (253 KB) LCMS (99 KB)

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

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

Ro 25-6981 Related Classifications

Neurological Disease

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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Ro 25-6981

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Other Forms of Ro 25-6981:

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6 Publications Citing Use of MCE Ro 25-6981

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References

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Complete Stock Solution Preparation Table

Ro 25-6981 Related Classifications

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