2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Sigma Receptor
  4. Roluperidone

Roluperidone  (Synonyms: CYR-101; MIN-101; MT-210)

Cat. No.: HY-19469 Purity: 99.86%
SDS COA Handling Instructions

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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).

For research use only. We do not sell to patients.

Roluperidone Chemical Structure

Roluperidone Chemical Structure

CAS No. : 359625-79-9

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Customer Review

Based on 1 publication(s) in Google Scholar

Roluperidone Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Roluperidone

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

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Sigma 1 Receptor Sigma 2 Receptor

  • Biological Activity

  • Purity & Documentation

  • References

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Description

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).

IC50 & Target[1]

5-HT2A Receptor

7.53 nM (Ki)

Sigma-2 Receptor

8.19 nM (Ki)

In Vitro

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.

Roluperidone Related Antibodies
Clinical Trial
Molecular Weight

366.43

Formula

C22H23FN2O2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C1N(CC2CCN(CC(C3=CC=C(F)C=C3)=O)CC2)CC4=C1C=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

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)

Preparing
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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 3 mg/mL (8.19 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.86%

SDS (252 KB)

COA (251 KB) HNMR (260 KB) LCMS (87 KB)

Handling Instructions (2659 KB)
References

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
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
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Roluperidone Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Roluperidone359625-79-9CYR-101 MIN-101 MT-210CYR101CYR 101MIN101MIN 101MIN-101MT210MT 210MT-2105-HT ReceptorSigma ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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