Roluperidone
Based on 1 publication(s) in Google Scholar
Roluperidone (CYR-101) is a novel cyclic amide derivative that has high equipotent affinities for 5-HT2A and sigma-2 receptors (Ki of 7.53 nM and 8.19 nM for 5-HT2A and sigma-2, respectively).
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- Pureté: 99.86%
- CAS No.: 359625-79-9
- Formule: C22H23FN2O2
- Masse moléculaire:366.43
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Stockage:Powder -20°C, 3 years , 4°C, 2 years
* The compound is unstable in solutions, freshly prepared is recommended.
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Roluperidone
MoreVoir tous les produits spécifiques à Isoform 5-HT Receptor
MoreVoir tous les produits spécifiques à Isoform Sigma Receptor
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Activité biologique
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5-HT2A Receptor 7.53 nM (Ki) |
5-HT2A Receptor |
Sigma-2 Receptor 8.19 nM (Ki) |
Roluperidone (CYR-101) also shows binding affinity for α1-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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 359625-79-9
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Appearance Solid
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Masse moléculaire 366.43
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Formule C22H23FN2O2
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Color White to yellow
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SMILES
O=C1N(CC2CCN(CC(C3=CC=C(F)C=C3)=O)CC2)CC4=C1C=CC=C4
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Synonyms
CYR-101; MIN-101; MT-210
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years * The compound is unstable in solutions, freshly prepared is recommended.
Publications (1)
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Journal Impact Factor
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Most Recent
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Eur J Pharmacol
Sigma-1 receptor agonist properties that mediate the fast-onset antidepressant effect of hypidone hydrochloride (YL-0919). [Abstract]2023 May 5:946:175647. PMID: 36898424
Solvant et solubilité
DMSO : 33.33 mg/mL (90.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (8.19 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.82 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * The compound is unstable in solutions, freshly prepared is recommended.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.7290 mL | 13.6452 mL | 27.2903 mL | 68.2259 mL |
| 5 mM | 0.5458 mL | 2.7290 mL | 5.4581 mL | 13.6452 mL | |
| 10 mM | 0.2729 mL | 1.3645 mL | 2.7290 mL | 6.8226 mL | |
| 15 mM | 0.1819 mL | 0.9097 mL | 1.8194 mL | 4.5484 mL | |
| 20 mM | 0.1365 mL | 0.6823 mL | 1.3645 mL | 3.4113 mL | |
| 25 mM | 0.1092 mL | 0.5458 mL | 1.0916 mL | 2.7290 mL | |
| 30 mM | 0.0910 mL | 0.4548 mL | 0.9097 mL | 2.2742 mL | |
| 40 mM | 0.0682 mL | 0.3411 mL | 0.6823 mL | 1.7056 mL | |
| 50 mM | 0.0546 mL | 0.2729 mL | 0.5458 mL | 1.3645 mL | |
| 60 mM | 0.0455 mL | 0.2274 mL | 0.4548 mL | 1.1371 mL | |
| 80 mM | 0.0341 mL | 0.1706 mL | 0.3411 mL | 0.8528 mL |
Roluperidone Related Classifications
HY-19469 Related Classifications
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