Roluperidone (CYR-101) (Synonyms: CYR-101; MIN-101; MT-210) |
| رقم الكتالوجGC30206 |
Roluperidone (CYR-101) (CYR-101) هو مشتق دوري جديد للأميد يحتوي على ارتباطات متوازنة عالية لمستقبلات 5-HT2A و Sigma-2 (Ki من 7.53 نانومتر و 8.19 نانومتر لـ 5-HT2A و سيجما -2 ، على التوالي) .
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 359625-79-9
Sample solution is provided at 25 µL, 10mM.
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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).
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].
[1]. Davidson M, et al. Efficacy and Safety of MIN-101: A 12-Week Randomized, Double-Blind, Placebo-Controlled Trial of a New Drug in Development for the Treatment of Negative Symptoms in Schizophrenia. Am J Psychiatry. 2017 Jul 28:appiajp201717010122.
| Cas No. | 359625-79-9 | SDF | |
| المرادفات | CYR-101; MIN-101; MT-210 | ||
| Canonical SMILES | O=C1N(CC2CCN(CC(C3=CC=C(F)C=C3)=O)CC2)CC4=C1C=CC=C4 | ||
| Formula | C22H23FN2O2 | M.Wt | 366.43 |
| الذوبان | DMSO : 33.33 mg/mL (90.96 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.729 mL | 13.6452 mL | 27.2903 mL |
| 5 mM | 0.5458 mL | 2.729 mL | 5.4581 mL |
| 10 mM | 0.2729 mL | 1.3645 mL | 2.729 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)
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