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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Ro 25-6981 is a highly potent and selective blocker of N-methyl-D-aspartate receptors containing the NR2B subunit. Ro 25-6981 inhibited 3H-MK-801 binding to rat forebrain membranes in a biphasic manner with IC50 of 0.003 microM and 149 microM for high- (about 60%) and low-affinity sites, respectively. NMDA receptor subtypes expressed in Xenopus oocytes were blocked with IC50 of 0.009 microM and 52 microM for the subunit combinations NR1C & NR2B and NR1C & NR2A, respectively, which indicated a >5000-fold selectivity. References: Szczurowska E, Mareš P. 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;111-8. doi: 10.1016/j.brainresbull.2014.11.001. Epub 2014 Nov 11. PubMed PMID: 25446739.
| ln Vivo |
Rats lesioned with 6-hydroxydopamine (6-OHDA) exhibit counterrotation when administered intraperitoneally with Ro 25-6981 (0.39-12.5 mg/kg); nevertheless, normal rats do not exhibit any stimulation of locomotion [1]. In early postnatal development in rats, Ro 25-6981 (1.3 mg/kg; i.p.) shows age- and activation-dependent anticonvulsant effects [2]. Intrathecal injection of Ro 25-6981 (800 µg) significantly lowers postoperative hyperalgesia and has a considerable analgesic impact on incision pain in rats [3].
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| Animal Protocol |
Animal/Disease Models: 6-OHDA injured rat [1]
Doses: 0.39-12.5 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Dose-dependent induction of opposite tight nasal-caudal rotation and weak co-directional rotation response, indicating Effect of mildly non-specific stimulating compounds. Animal/Disease Models: Male albino rats of Wistar strain [2] Doses: 1, 3 mg/kg Route of Administration: Ip Experimental Results: N1-P2 amplitude was Dramatically diminished at the higher stimulation intensity of 3 mg/kg, and demonstrated Age- and activation-dependent anticonvulsant effects in early postnatal development. |
| References |
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| Additional Infomation |
Ro 25-6981 is a member of the class of piperidines that is 4-benzylpiperidine substituted by a 3-hydroxy-3-(4-hydroxyphenyl)-2-methylpropyl group at position 1 (the 1R,2S-stereoisomer). It is a potent antagonist of the GluN2B subunit of the N-methyl-D-aspartate (NMDA) receptor. It has a role as a NMDA receptor antagonist, an anticonvulsant, an antidepressant and a neuroprotective agent. It is a member of piperidines, a member of phenols, a secondary alcohol, a tertiary amino compound and a member of benzenes. It is a conjugate base of a Ro 25-6981(1+).
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| Molecular Formula |
C22H29NO2
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|---|---|
| Molecular Weight |
339.479
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| Exact Mass |
339.219
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| CAS # |
169274-78-6
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| Related CAS # |
Ro 25-6981 Maleate;1312991-76-6;Ro 25-6981 hydrochloride;919289-58-0
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| PubChem CID |
6604887
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| Appearance |
White to off-white solid powder
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| Boiling Point |
703.7ºC at 760mmHg
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| Flash Point |
379.4ºC
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| Vapour Pressure |
2.52E-11mmHg at 25°C
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| Index of Refraction |
1.587
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| LogP |
3.666
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
25
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| Complexity |
366
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C[C@@H](CN1CCC(CC1)CC2=CC=CC=C2)[C@H](C3=CC=C(C=C3)O)O
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| InChi Key |
WVZSEUPGUDIELE-HTAPYJJXSA-N
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| InChi Code |
InChI=1S/C22H29NO2/c1-17(22(25)20-7-9-21(24)10-8-20)16-23-13-11-19(12-14-23)15-18-5-3-2-4-6-18/h2-10,17,19,22,24-25H,11-16H2,1H3/t17-,22+/m0/s1
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| Chemical Name |
4-((1R,2S)-3-(4-benzylpiperidin-1-yl)-1-hydroxy-2-methylpropyl)phenol
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| Synonyms |
Ro 25-6981 Ro25-6981 Ro-25-6981 Ro-256981 Ro 256981 Ro256981 Ro 25-6981 free base
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9457 mL | 14.7284 mL | 29.4568 mL | |
| 5 mM | 0.5891 mL | 2.9457 mL | 5.8914 mL | |
| 10 mM | 0.2946 mL | 1.4728 mL | 2.9457 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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