2. Neuronal Signaling
  3. Sigma Receptor
  4. (±)-Vesamicol hydrochloride

(±)-Vesamicol hydrochloride  (Synonyms: (±)-AH5183 hydrochloride)

Cat. No.: HY-B1813A Purity: 99.81%
COA Handling Instructions

Molarity Calculator

(±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a Ki of 2 nM. (±)-Vesamicol hydrochloride also displays high affinity for σ1 and σ2 receptors with Kis of 26 nM and 34 nM, respectively.

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

(±)-Vesamicol hydrochloride Chemical Structure

(±)-Vesamicol hydrochloride Chemical Structure

CAS No. : 120447-62-3

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Based on 1 publication(s) in Google Scholar

Other Forms of (±)-Vesamicol hydrochloride:

(±)-Vesamicol hydrochloride Related Antibodies

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Description

(±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a Ki of 2 nM. (±)-Vesamicol hydrochloride also displays high affinity for σ1 and σ2 receptors with Kis of 26 nM and 34 nM, respectively[1][2].

IC50 & Target

Sigma 1 Receptor

 

Sigma 2 Receptor

 

In Vitro

The pharmacological actions of (±)-Vesamicol have been attributed to inhibition of acetylcholine transport into synaptic vesicles and the subsequent quantal release of acetylcholine[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

(±)-Vesamicol hydrochloride Related Antibodies
In Vivo

(±)-Vesamicol (3 mg/kg; intraperitoneal injection; once; male Wistar rats) treatment increases the levels of cytosolic acetylcholine (ACh) in all regions of the brain, while those of vesicular ACh decreased in all regions except for the striatum[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar rats (120-300 g)[2]
Dosage: 3 mg/kg
Administration: Intraperitoneal injection; once
Result: The levels of cytosolic acetylcholine (ACh) increased in all regions of the brain, while those of vesicular ACh decreased in all regions except for the striatum.
Molecular Weight

295.85

Formula

C17H26ClNO
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]1[C@H](N2CCC(C3=CC=CC=C3)CC2)CCCC1.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 14 mg/mL (47.32 mM; ultrasonic and warming and heat to 60°C; 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 3.3801 mL 16.9005 mL 33.8009 mL
5 mM 0.6760 mL 3.3801 mL 6.7602 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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: ≥ 2.08 mg/mL (7.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (7.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 99.81%

COA (250 KB) HNMR (283 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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3801 mL 16.9005 mL 33.8009 mL 84.5023 mL
5 mM 0.6760 mL 3.3801 mL 6.7602 mL 16.9005 mL
10 mM 0.3380 mL 1.6900 mL 3.3801 mL 8.4502 mL
15 mM 0.2253 mL 1.1267 mL 2.2534 mL 5.6335 mL
20 mM 0.1690 mL 0.8450 mL 1.6900 mL 4.2251 mL
25 mM 0.1352 mL 0.6760 mL 1.3520 mL 3.3801 mL
30 mM 0.1127 mL 0.5633 mL 1.1267 mL 2.8167 mL
40 mM 0.0845 mL 0.4225 mL 0.8450 mL 2.1126 mL
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(±)-Vesamicol hydrochloride 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:

(±)-Vesamicol120447-62-3(±)-AH5183Sigma ReceptorVesicularacetylcholinetransporternerveσ1-receptorσ2-receptorInhibitorinhibitorinhibit

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