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Cat. No.: HY-149274

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Sigma-1 receptor antagonist 4

Sigma-1 receptor antagonist 4 (Compound 32) is a potent σ1R antagonist that significantly enhances the analgesic effect of morphine and rescues morphine-induced analgesic tolerance, with potential to prevent morphine tolerance.

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

CAS No.: 3041072-11-8
Formula: C₂₂H₂₆N₂O
Molecular Weight:334.45

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (268 KB)

Sigma-1 receptor antagonist 4 Chemical Structure

CAS No.: 3041072-11-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Solvent & Solubility
- In Vivo
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 19.1 ± 0.6 nM (σ1R)^[1]

All Sigma Receptor Isoforms :

In Vivo

Sigma-1 receptor antagonist 4 (0–60 mg/kg; i.p.; single dose) dose-dependently enhances morphine-induced analgesia within a dose of 40 mg/kg^[1].
Sigma-1 receptor antagonist 4 (30 mg/kg; i.p.; single dose) potentiates antinociception via enhancing the morphineinduced MOR agonism^[1].

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

Animal Model:

Mouse model^[1]
Dosage:

10, 20, 30, 40, 50, 60 mg/kg
Administration:

i.p.; dissolved in saline with 30% PEG300 and 5% DMSO; measured the percentage of maximal possible effect (% MPE)after 30 min
Result:

Dose-dependently enhanced morphine-induced analgesia within a dose of 40 mg/kg. Potentiated antinociception via enhancing the morphine-induced MOR agonism.

Chemical Information

CAS No. 3041072-11-8
Molecular Weight 334.45
Formula C₂₂H₂₆N₂O
SMILES

CC1=CC=C(C=C1)CCCN2CC3(C2)CC(N(C3)C4=CC=CC=C4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

View the Complete Stock Solution Preparation Table

In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

Protocol 1

dissolved in saline with 30% PEG300 and 5% DMSO

In Vivo Dissolution Calculator

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.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Fu K, et al. 2,6-diazaspiro[3.4]octan-7-one derivatives as potent sigma-1 receptor antagonists that enhanced the antinociceptive effect of morphine and rescued morphine tolerance. Eur J Med Chem. 2023 Mar 5;249:115178. [Content Brief]

Calculators

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

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Solvent & Solubility
- In Vivo
Purity & Documentation
References

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Sigma-1 receptor antagonist 4

All Sigma Receptor Isoforms