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Purity: ≥98%
Roluperidone (formerly also known as CYR-101, MIN-101, CYR101, and MT-210) is a novel and potent cyclic amide derivative with-schizophrenia effects. It has strong equipotent affinities for sigma-2 and 5-HT2A receptors, with Ki values of 8.19 nM and 7.53 nM for sigma-2 and 5-HT2A, respectively. Being an antagonist of both sigma 2 and 5-HT2A receptors, it may find application in the management of schizophrenia.
| Targets |
5-HT2A Receptor ( Ki = 7.53 nM ); Sigma-2 Receptor ( Ki = 8.19 nM )
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| ln Vitro |
Roluperidone (CYR-101) additionally exhibits α1-adrenergic receptor binding affinity, but little to no affinity for histamine, cholinergic, or muscarinic receptors. Despite the lack of affinity for pre- or postsynaptic dopaminergic receptors, roluperidone (CYR-101) is likely associated with sigma-2 receptors that are involved in the modulation of glutamatergic and dopaminergic pathways as well as calcium neuronal modulation[1].
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| References |
| Molecular Formula |
C22H23FN2O2
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|---|---|
| Molecular Weight |
366.4286
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| Exact Mass |
366.17
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| Elemental Analysis |
C, 72.11; H, 6.33; F, 5.18; N, 7.64; O, 8.73
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| CAS # |
359625-79-9
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| Appearance |
Solid powder
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| SMILES |
C1CN(CCC1CN2CC3=CC=CC=C3C2=O)CC(=O)C4=CC=C(C=C4)F
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| InChi Key |
RNRYULFRLCBRQS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H23FN2O2/c23-19-7-5-17(6-8-19)21(26)15-24-11-9-16(10-12-24)13-25-14-18-3-1-2-4-20(18)22(25)27/h1-8,16H,9-15H2
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| Chemical Name |
2-[[1-[2-(4-fluorophenyl)-2-oxoethyl]piperidin-4-yl]methyl]-3H-isoindol-1-one
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| Synonyms |
MT-210; MIN101; CYR-101; MT 210; MIN 101; CYR 101; MT210; MIN-101; CYR101; Roluperidone
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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 Note: This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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) |
DMSO: ~33.33 mg/mL (~91.0 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (8.19 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3 mg/mL (8.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.82 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7290 mL | 13.6452 mL | 27.2903 mL | |
| 5 mM | 0.5458 mL | 2.7290 mL | 5.4581 mL | |
| 10 mM | 0.2729 mL | 1.3645 mL | 2.7290 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06107803 | Recruiting | Drug: Roluperidone 64 mg Drug: Olanzapine 10 MG |
Negative Symptoms in Schizophrenia |
Minerva Neurosciences | October 13, 2023 | Phase 1 |
| NCT03397134 | Completed | Drug: Placebo Oral Tablet Drug: Roluperidone 32 mg |
Negative Symptoms of Schizophrenia |
Minerva Neurosciences | December 15, 2017 | Phase 3 |
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