SCS
Based on 1 Customer Validation
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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- Pureté: 98.68%
- CAS No.: 3232-36-8
- Formule: C14H12N2O3
- Masse moléculaire:256.26
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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]
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Cell Line
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Type | Value | Description | References |
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| J774 | IC50 |
1219.46 μM
Compound: 20, H2sashz
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Cytotoxicity against mouse J774 cells after 24 hrs by resazurin assay
Cytotoxicity against mouse J774 cells after 24 hrs by resazurin assay
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[PMID: 20163897] |
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.
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.
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Animal Model:BALB/c mice; tonic, phasic and Capsaicin (HY-10448) nociception model[2]
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Dosage:10, 25, 50, and 75 mg/kg
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Administration:IP, single dose
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Result:Produced a significant protection on tonic, phasic and capsaicin nociception in a dose-dependent manner.
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Animal Model:BALB/c mice, Oxaliplatin (HY-17371)-induced neuropathic nociception model[2]
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Dosage:50 and 75 mg/kg
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Administration:IP, single dose
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Result:Significantly attenuated the paw withdrawal threshold changes associated with Oxaliplatin. Significantly increased the percent antinociception during 30-120 min.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 3232-36-8
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Appearance Solid
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Masse moléculaire 256.26
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Formule C14H12N2O3
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Color Off-white to yellow
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SMILES
O=C(N/N=C/C1=CC=CC=C1O)C2=CC=CC=C2O
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Synonyms
Salicylidene salicylhydrazide
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Thompson SA, et al. Salicylidene salicylhydrazide, a selective inhibitor of beta 1-containing GABAA receptors. Br J Pharmacol. 2004 May;142(1):97-106. [Content Brief]
[2]. Rukh L, et al. Efficacy assessment of salicylidene salicylhydrazide in chemotherapy associated peripheral neuropathy. Eur J Pharmacol. 2020 Dec 5;888:173481. [Content Brief]
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 |
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| 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 |
SCS Related Classifications
HY-103528 Related Classifications
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