2. Neuronal Signaling
  3. Sigma Receptor
  4. S1R agonist 1

S1R agonist 1 (Compound 6b) is a selective S1R agonist with Kis of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 exhibits neuroprotection against ROS and NMDA-induced neurotoxicity.

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S1R agonist 1 Chemical Structure

S1R agonist 1 Chemical Structure

CAS No. : 193354-70-0

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Based on 1 publication(s) in Google Scholar

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S1R agonist 1 Related Antibodies

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Description

S1R agonist 1 (Compound 6b) is a selective S1R agonist with Kis of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 exhibits neuroprotection against ROS and NMDA-induced neurotoxicity[1].

IC50 & Target[1]

Sigma 1 Receptor

0.93 nM (Ki)

Sigma 2 Receptor

72 nM (Ki)

In Vitro

S1R agonist 1 (Compound 6b; 0.1-5 μM) significantly increases the nerve growth factor (NGF) induced neurite outgrowth at all the tested concentrations in a dose-dependent manner in PC12 cell lines[1].
S1R agonist 1 (24 h) significantly prevents cell damage induced by Rotenone (HY-B1756) when tested at the concentration of 1 μM in SHSY5Y cells[1].
S1R agonist 1 (0.1-5 μM; 24 h) demonstrates a neuroprotective effect against NMDA stimuli in SHSY5Y cells[1].
S1R agonist 1 (0-10 μM; 24-72 h) shows no cytotoxicity against A549, LoVo and Panc-1 cells[1].

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

S1R agonist 1 Related Antibodies
In Vivo

S1R agonist 1 (Compound 6b; 0.1-50 μM; 120 h) induces the death of 4 Zebrafish embryos out of 8 at 10 μM[1].

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

295.42

Formula

C20H25NO
CAS No.
Appearance

Liquid (Density: 1.048±0.06 g/cm3)

Color

Colorless to light yellow

SMILES

C1(OCCN2CCC(CC2)CC3=CC=CC=C3)=CC=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (338.50 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 3.3850 mL 16.9251 mL 33.8501 mL
5 mM 0.6770 mL 3.3850 mL 6.7700 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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.46 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 (8.46 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)

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 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
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. 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 3.3850 mL 16.9251 mL 33.8501 mL 84.6253 mL
5 mM 0.6770 mL 3.3850 mL 6.7700 mL 16.9251 mL
10 mM 0.3385 mL 1.6925 mL 3.3850 mL 8.4625 mL
15 mM 0.2257 mL 1.1283 mL 2.2567 mL 5.6417 mL
20 mM 0.1693 mL 0.8463 mL 1.6925 mL 4.2313 mL
25 mM 0.1354 mL 0.6770 mL 1.3540 mL 3.3850 mL
30 mM 0.1128 mL 0.5642 mL 1.1283 mL 2.8208 mL
40 mM 0.0846 mL 0.4231 mL 0.8463 mL 2.1156 mL
50 mM 0.0677 mL 0.3385 mL 0.6770 mL 1.6925 mL
60 mM 0.0564 mL 0.2821 mL 0.5642 mL 1.4104 mL
80 mM 0.0423 mL 0.2116 mL 0.4231 mL 1.0578 mL
100 mM 0.0339 mL 0.1693 mL 0.3385 mL 0.8463 mL
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S1R agonist 1 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:

S1R agonist 1193354-70-0Sigma ReceptorSHSY5YPC12Inhibitorinhibitorinhibit

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