AChE-IN-117
AChE-IN-117 is an AChE/nAChR inhibitor with larvicidal activity against Culex pipiens third-instar larvae. AChE-IN-117 forms stable catalytic site interactions to disrupt cholinergic signaling. AChE-IN-117 binds to its receptor via hydrogen bonding and π-cation interactions to interfere with cholinergic synaptic transmission. AChE-IN-117 induces neurotoxic symptoms including hyperactivity, erratic movement, tremors, paralysis, and larval mortality. AChE-IN-117 can be used for the research of mosquito-borne infectious diseases.
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- 화학식: C15H11N7O2S
- 분자량:353.36
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
AChE |
In Vitro
AChE-IN-117 (compound 7) (11.25-90 µg/mL; 24 h) potently kills third-instar Culex pipiens larvae with an LC50 of 0.16 µg/mL[1].
AChE-IN-117 binds strongly to homology-modeled Culex pipiens AChE with a binding affinity of -6.70 kcal/mol, forming stable interactions with key active-site residues[1].
AChE-IN-117 binds to homology-modeled Culex pipiens nAChR with a binding affinity of -5.78 kcal/mol, forming key interactions with critical receptor residues[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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분자량 353.36
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화학식 C15H11N7O2S
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SMILES
CC1=NN(C2=C1C(C3=CC=C(C=C3)[N+]([O-])=O)=C(C(N)=N2)C#N)C(N)=S
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Neurotoxicity Study
This protocol assesses in vitro neurotoxicity by combining neuronal viability, mitochondrial/metabolic activity, neurite outgrowth, and optional neuronal network function readouts. Calcein-AM or resazurin/PrestoBlue readouts estimate viable or metabolically active cells; βIII-tubulin immunofluorescence detects neuronal morphology and neurite networks; TMRE detects mitochondrial membrane potential; and MEA recordings detect functional changes in neuronal network activity.
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Synaptic current patch-clamp recording in brain slices
Whole-cell patch-clamp recording in acute brain slices measures membrane current from visually identified neurons while preserving part of the local synaptic circuit; in voltage clamp, postsynaptic currents are generated by synaptic receptor-channel activation and are recorded as inward or outward currents at a defined holding potential. Miniature synaptic currents are recorded during action-potential blockade with tetrodotoxin, whereas evoked synaptic currents are generated by pathway stimulation and isolated pharmacologically as EPSCs or IPSCs.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AChE-IN-117 Related Classifications
HY-184140 Related Classifications
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Keywords
- AChE-IN-117
- Insecticide
- nAChR
- Cholinesterase (ChE)
- cholinergic synaptic transmission
- mosquito-borne infectious diseases
- receptor residues
- nicotinic acetylcholine receptor
- cholinergic signaling
- acetylcholinesterase
- Culex pipiens
- third-instar larvae
- active-site residues
- neurotoxic symptoms
- Inhibitor
- inhibitor
- inhibit