σ1 Receptor antagonist-1

Name: σ1 Receptor antagonist-1
Brand: MedChemExpress
SKU: HY-10815
Rating: 4.5 (1 reviews)

Cat. No.: HY-10815 Purity: 99.70%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pK_i=10.28). σ1 Receptor antagonist-1 inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells.

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

σ1 Receptor antagonist-1 Chemical Structure

CAS No. : 1204401-49-9

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 115	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 115	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 105	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 352	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 572	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 935	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE σ1 Receptor antagonist-1

•Cells. 2023 Jan 3;12(1):197. [Abstract]

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Sigma 1 Receptor

In Vitro

σ1 Receptor antagonist-1 (compound 9) (10 μM; 48 hours) inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells^[1].

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

Cell Cycle Analysis^[1]

Cell Line:	MCF-7/ADR, MCF-7 cells
Concentration:	10 μM
Incubation Time:	48 hours
Result:	Increased the number of cells in G0/G1 (27.8%) and decreased those in S phase (46.7%), in a sigma 1-dependent manner. It selectively affects the high sigma 1 receptor expressing MCF-7/ADR but not the low sigma 1 receptor expressing MCF-7 cells.

In Vivo

Pretreatment withσ1 Receptor antagonist-1 (1 mg/kg; s.c.) significantly increases the anti-nociceptive effect produces by morphine over the entire time course starting at 60 min^[1].

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

Animal Model:	Male CD-1 mice^[1]
Dosage:	1 mg/kg
Administration:	S.c.
Result:	Significantly increased the anti-nociceptive effect produced by morphine over the entire time course starting at 60 min.

Molecular Weight

337.48

Formula

C₂₁H₂₃NOS

CAS No.

1204401-49-9

Appearance

Solid

Color

Light yellow to light brown

SMILES

O=C1CC(C2CCN(CC3=CC=CC=C3)CC2)SC4=CC=CC=C41

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (296.31 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	2.9631 mL	14.8157 mL	29.6314 mL
5 mM	0.5926 mL	2.9631 mL	5.9263 mL
10 mM	0.2963 mL	1.4816 mL	2.9631 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. 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.41 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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)

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 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: 99.70%

Select Batch:

Data Sheet (273 KB) SDS (252 KB)

COA (247 KB) HNMR (274 KB) LCMS (270 KB)

Handling Instructions (2659 KB)

References

[1]. Piergentili A, et al. Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane. J Med Chem. 2010;53(3):1261-1269. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.9631 mL	14.8157 mL	29.6314 mL	74.0785 mL
	5 mM	0.5926 mL	2.9631 mL	5.9263 mL	14.8157 mL
	10 mM	0.2963 mL	1.4816 mL	2.9631 mL	7.4078 mL
	15 mM	0.1975 mL	0.9877 mL	1.9754 mL	4.9386 mL
	20 mM	0.1482 mL	0.7408 mL	1.4816 mL	3.7039 mL
	25 mM	0.1185 mL	0.5926 mL	1.1853 mL	2.9631 mL
	30 mM	0.0988 mL	0.4939 mL	0.9877 mL	2.4693 mL
	40 mM	0.0741 mL	0.3704 mL	0.7408 mL	1.8520 mL
	50 mM	0.0593 mL	0.2963 mL	0.5926 mL	1.4816 mL
	60 mM	0.0494 mL	0.2469 mL	0.4939 mL	1.2346 mL
	80 mM	0.0370 mL	0.1852 mL	0.3704 mL	0.9260 mL
	100 mM	0.0296 mL	0.1482 mL	0.2963 mL	0.7408 mL