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Roluperidone (CYR-101), a novel cyclic amide derivative, exhibits high equipotent affinities for 5-HT2A and σ2 receptors with Ki values of 7.53 nM and 8.19 nM, respectively.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $30 | In Stock | In Stock | |
| 5 mg | $47 | In Stock | In Stock | |
| 10 mg | $79 | In Stock | In Stock | |
| 25 mg | $158 | In Stock | In Stock | |
| 50 mg | $257 | In Stock | In Stock | |
| 100 mg | $395 | In Stock | In Stock |
| Description | Roluperidone (CYR-101), a novel cyclic amide derivative, exhibits high equipotent affinities for 5-HT2A and σ2 receptors with Ki values of 7.53 nM and 8.19 nM, respectively. |
| Targets&IC50 | σ2 receptor:8.19 nM(ki), 5-HT2A:7.53 nM(ki) |
| In vitro | Roluperidone shows binding affinity for α1-adrenergic receptors. Which low or no affinity for muscarinic, cholinergic, and histaminergic receptors. Although Roluperidone (CYR-101) has no affinities for pre- or postsynaptic dopaminergic receptors, it is probable that sigma-2 receptors are implicated in the modulation of dopamine and glutamatergic pathways and in calcium neuronal modulation[1]. |
| Synonyms | MT-210, MIN-101, CYR-101 |
| Molecular Weight | 366.43 |
| Formula | C22H23FN2O2 |
| Cas No. | 359625-79-9 |
| Smiles | Fc1ccc(cc1)C(=O)CN1CCC(CN2Cc3ccccc3C2=O)CC1 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | H2O: < 0.1 mg/mL (insoluble) DMSO: 33.33 mg/mL (90.96 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.5 mg/mL (6.82 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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