| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
nAChR[1]
TQS targets the α7 nicotinic acetylcholine receptor (α7 nAChR). As a positive allosteric modulator (PAM), it does not directly activate the receptor but binds to a site distinct from the orthosteric (agonist) binding site. It enhances the receptor's response to acetylcholine by increasing channel open time and reducing desensitization. This allosteric modulation leads to a sustained potentiation of cholinergic signaling. |
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| ln Vitro |
In vitro, TQS enhances α7 nAChR-mediated responses. Its Type II PAM activity is characterized by a unique ability to dramatically slow or nearly eliminate receptor desensitization and to reactivate desensitized channels, properties not shared by Type I PAMs. This mechanism leads to a more robust and sustained receptor activation upon agonist binding, which is crucial for its research applications.
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| ln Vivo |
TQS (1 or 4 mg/kg; ip) inhibits the production of CD11b mRNA and IκB mRNA caused by LPS and controls the morphological alterations of microglia in the hippocampus[1].
In vivo, TQS has been shown to reduce LPS-induced IκB and CD11b gene expression by targeting microglial α7 nAChR in the hippocampus. This is associated with a reduction in microglial activation related to hyperalgesia and mechanical allodynia. These findings support its use in studying neuroinflammatory pain and microglial responses. |
| Enzyme Assay |
Non-cell-based assays for TQS involve evaluating its binding and function on α7 nAChRs. Radioligand binding studies can determine its affinity for the allosteric site. Functional assays, such as electrophysiology (e.g., patch-clamp) on cells expressing α7 nAChRs, are used to measure the potentiation of acetylcholine-induced currents. The compound's ability to reduce desensitization is a key readout in these studies.
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| Cell Assay |
For in vitro cellular assays, cells expressing α7 nAChRs are treated with TQS. Its effects on receptor function are typically assessed by measuring calcium influx using fluorescent dyes (e.g., Fluo-4). Cells are pre-incubated with TQS and then stimulated with a sub-maximal concentration of an agonist like acetylcholine or choline. The potentiation of the calcium signal indicates PAM activity.
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| Animal Protocol |
Animal/Disease Models: Male C57BL/6J mice[1]
Doses: 1 or 4 mg/kg Route of Administration: Ip Experimental Results: decreased the expression of LPS-induced IκB mRNA, CD11b mRNA and regulated microglial morphological changes in the hippocampus. In vivo animal studies for TQS involve administering the compound to rodents in models of neuropathic pain. For example, in a model of LPS-induced neuroinflammation, TQS treatment led to a reduction in pain-related behaviors and a decrease in markers of microglial activation in the brain. This demonstrates its potential for studying conditions involving neuroinflammation. |
| ADME/Pharmacokinetics |
TQS has a molecular weight of 376.47 g/mol and a molecular formula of C22H20N2O2S. It is soluble in DMSO up to 240 mg/mL and can be formulated for in vivo use (e.g., 10% DMSO+40% PEG300+5% Tween 80+45% Saline). The powder should be stored at -20°C for up to 3 years. It is for research use only.
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| Toxicity/Toxicokinetics |
The toxicity profile of TQS is not extensively detailed. As a research compound, comprehensive toxicological data are not typically available. It is for research use only and not for human consumption. Standard safety precautions for handling chemical compounds should be followed.
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| References | |
| Additional Infomation |
TQS (CAS#: 353483-92-8) is a research tool used to study the α7 nAChR, particularly its role in neuroinflammation and pain. As a Type II PAM, its mechanism of action—reducing desensitization—makes it a distinct and valuable probe for understanding α7 nAChR function and for developing new therapeutic strategies for pain and inflammation.
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| Molecular Formula |
C22H20N2O2S
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|---|---|
| Molecular Weight |
376.47
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| Exact Mass |
376.125
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| CAS # |
353483-92-8
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| PubChem CID |
5038679
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
6.232
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
27
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| Complexity |
685
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C=CC2C1C(NC3=C2C=C(C=C3)S(=O)(=O)N)C4=CC=CC5=CC=CC=C54
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| InChi Key |
SIZWDJIHABLBSP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H20N2O2S/c23-27(25,26)15-11-12-21-20(13-15)17-8-4-10-19(17)22(24-21)18-9-3-6-14-5-1-2-7-16(14)18/h1-9,11-13,17,19,22,24H,10H2,(H2,23,25,26)
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| Chemical Name |
4-naphthalen-1-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 125 mg/mL (332.03 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.53 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.53 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6563 mL | 13.2813 mL | 26.5625 mL | |
| 5 mM | 0.5313 mL | 2.6563 mL | 5.3125 mL | |
| 10 mM | 0.2656 mL | 1.3281 mL | 2.6563 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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