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

S1R agonist 2 (Compound 8b) is a selective S1R agonist with Kis of 1.1 nM and 88 nM for S1R and S2R, respectively. S1R agonist 2 exhibits neuroprotection against ROS and NMDA-induced neurotoxicity.

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S1R agonist 2 Chemical Structure

S1R agonist 2 Chemical Structure

CAS No. : 150085-21-5

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Based on 1 publication(s) in Google Scholar

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S1R agonist 2 Related Antibodies

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Description

S1R agonist 2 (Compound 8b) is a selective S1R agonist with Kis of 1.1 nM and 88 nM for S1R and S2R, respectively. S1R agonist 2 exhibits neuroprotection against ROS and NMDA-induced neurotoxicity[1].

IC50 & Target[1]

Sigma 1 Receptor

1.1 nM (Ki)

Sigma 2 Receptor

88 nM (Ki)

In Vitro

S1R agonist 2 (Compound 8b; 0.1-5 μM) significantly increases the nerve growth factor (NGF) induced neurite outgrowth at all the tested concentrations in a dose-dependent manner[1].
S1R agonist 2 (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 2 (0.1-5 μM; 24 h) demonstrates a neuroprotective effect against NMDA stimuli in SHSY5Y cells[1].
S1R agonist 2 (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 2 Related Antibodies
In Vivo

S1R agonist 2 (Compound 8b; 0.1-50 μM; 120 h) does not induce embryo death (100% of embryos alive) at 10 μM, but induces the death of all zebrafish embryo at the highest dose tested (50 μM)[1].

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

309.45

Formula

C21H27NO
CAS No.
Appearance

Liquid (Density: 1.037±0.06 g/cm3)

Color

Colorless to light yellow

SMILES

C1(OCCCN2CCC(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 : 200 mg/mL (646.31 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 3.2315 mL 16.1577 mL 32.3154 mL
5 mM 0.6463 mL 3.2315 mL 6.4631 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)

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

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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: ≥ 2.5 mg/mL (8.08 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 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: ≥ 2.5 mg/mL (8.08 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.
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 3.2315 mL 16.1577 mL 32.3154 mL 80.7885 mL
5 mM 0.6463 mL 3.2315 mL 6.4631 mL 16.1577 mL
10 mM 0.3232 mL 1.6158 mL 3.2315 mL 8.0788 mL
15 mM 0.2154 mL 1.0772 mL 2.1544 mL 5.3859 mL
20 mM 0.1616 mL 0.8079 mL 1.6158 mL 4.0394 mL
25 mM 0.1293 mL 0.6463 mL 1.2926 mL 3.2315 mL
30 mM 0.1077 mL 0.5386 mL 1.0772 mL 2.6929 mL
40 mM 0.0808 mL 0.4039 mL 0.8079 mL 2.0197 mL
50 mM 0.0646 mL 0.3232 mL 0.6463 mL 1.6158 mL
60 mM 0.0539 mL 0.2693 mL 0.5386 mL 1.3465 mL
80 mM 0.0404 mL 0.2020 mL 0.4039 mL 1.0099 mL
100 mM 0.0323 mL 0.1616 mL 0.3232 mL 0.8079 mL
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S1R agonist 2 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 2150085-21-5Sigma ReceptorSHSY5YPC12Inhibitorinhibitorinhibit

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