1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. SCS

SCS  (Synonyms: Salicylidene salicylhydrazide)

Cat. No.: HY-103528 Purity: 99.64%
Handling Instructions Technical Support

SCS (Salicylidene salicylhydrazide) is a potent, allosteric and selective inhibitor of β1-containing GABAA receptors with an IC50 of 32 nM against α2β1γ1θ by VIPR measurement. SCS is also a chelator of metal ions.

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SCS

SCS Chemical Structure

CAS No. : 3232-36-8

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

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Description

SCS (Salicylidene salicylhydrazide) is a potent, allosteric and selective inhibitor of β1-containing GABAA receptors with an IC50 of 32 nM against α2β1γ1θ by VIPR measurement. SCS is also a chelator of metal ions[1].

IC50 & Target

IC50: 32 nM (α2β1γ1θ; by VIPR measurement)
IC50: 4.5 nM (α2β1γ1θ), 5.3 nM (α2β1γ1), 7.9 nM (α1β1γ2s) (Measured by using whole-cell patch clamp)[1]

Cellular Effect
Cell Line Type Value Description References
J774 IC50
1219.46 μM
Compound: 20, H2sashz
Cytotoxicity against mouse J774 cells after 24 hrs by resazurin assay
Cytotoxicity against mouse J774 cells after 24 hrs by resazurin assay
[PMID: 20163897]
In Vitro

SCS (0.1 nM-3 μM) produces a concentration-dependent inhibition of GABA EC20 currents recorded from Ltk- cells expressing α2β1γ1θ, α2β1γ1 and α1β1γ2s receptors compared with α2β3γ2s and α1β2γ2s receptors upon which SCS has no effect[1].
Inhibition by SCS is not voltage or use dependent[1].
Structural determinants necessary for the inhibition of GABAA receptors by SCS are located within the region arginine 238 and glycine 335 of the β1 subunit. T255 and I308 of the β1 subunit are required for inhibition by SCS[1].

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

In Vivo

SCS (Salicylidene salicylhydrazide; 500-1000 mg/kg, i.p. or 800-1000 mg/kg, oral) produces abdominal constrictions in mice[2].
SCS (10-75 mg/kg; i.p.; once) shows antinociceptive activity against tonic, phasic and Capsaicin (HY-10448) nociception in mice[2].
SCS (10-75 mg/kg; i.p.; once) shows anti-inflammatory activity in mice[2]. SCS (50 and 75 mg/kg; i.p.; once) shows antinociceptive activity against neuropathic nociception[2].

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

Animal Model: BALB/c mice; tonic, phasic and Capsaicin (HY-10448) nociception model[2]
Dosage: 10, 25, 50, and 75 mg/kg
Administration: IP, single dose
Result: Produced a significant protection on tonic, phasic and capsaicin nociception in a dose-dependent manner.
Animal Model: BALB/c mice, Oxaliplatin (HY-17371)-induced neuropathic nociception model[2]
Dosage: 50 and 75 mg/kg
Administration: IP, single dose
Result: Significantly attenuated the paw withdrawal threshold changes associated with Oxaliplatin. Significantly increased the percent antinociception during 30-120 min.
Clinical Trial
Molecular Weight

256.26

Formula

C14H12N2O3

CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(N/N=C/C1=CC=CC=C1O)C2=CC=CC=C2O

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 : 5.56 mg/mL (21.70 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 3.9023 mL 19.5114 mL 39.0229 mL
5 mM 0.7805 mL 3.9023 mL 7.8046 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
=
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

×
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: ≥ 0.56 mg/mL (2.19 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.56 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.6 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% Corn Oil

    Solubility: ≥ 0.56 mg/mL (2.19 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.56 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 (5.6 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

Purity: 99.64%

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 3.9023 mL 19.5114 mL 39.0229 mL 97.5572 mL
5 mM 0.7805 mL 3.9023 mL 7.8046 mL 19.5114 mL
10 mM 0.3902 mL 1.9511 mL 3.9023 mL 9.7557 mL
15 mM 0.2602 mL 1.3008 mL 2.6015 mL 6.5038 mL
20 mM 0.1951 mL 0.9756 mL 1.9511 mL 4.8779 mL
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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.

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