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[CAS NO. 359625-79-9] Roluperidone
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-19469 |
| Brand: | MCE |
| CAS: | 359625-79-9 |
Overview
| MDL | MFCD28502826 |
|---|---|
| Molecular Weight | 366.43 |
| Molecular Formula | C22H23FN2O2 |
| SMILES | O=C1N(CC2CCN(CC(C3=CC=C(F)C=C3)=O)CC2)CC4=C1C=CC=C4 |
Summary
Roluperidone (CYR-101) is a novel cyclic amide derivative that has high equipotent affinities for 5-HT 2A and sigma-2 receptors ( K i of 7.53 nM and 8.19 nM for 5-HT 2A and sigma-2, respectively).
IC50 & Target
|
5-HT 2A Receptor 7.53 nM (Ki) |
Sigma-2 Receptor 8.19 nM (Ki) |
In Vitro
Roluperidone (CYR-101) also shows binding affinity for α 1 -adrenergic receptors but 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, as well as in calcium neuronal modulation [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02232529 | Minerva Neurosciences |
Schizophrenia
|
September 2014 | Phase 1 |
| NCT00861796 | Cyrenaic Pharmaceuticals |
Schizophrenia
|
March 2008 | Phase 2 |
| NCT03038646 | Minerva Neurosciences |
Healthy Subjects
|
November 30, 2016 | Phase 1 |
| NCT03397134 | Minerva Neurosciences |
Negative Symptoms of Schizophrenia
|
December 15, 2017 | Phase 3 |
| NCT03072056 | Minerva Neurosciences |
Healthy Subjects
|
January 9, 2017 | Phase 1 |
Appearance
Solid
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
DMSO : 33.33 mg/mL ( 90.96 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
Synonyms
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