BChE reactivator-1
BChE reactivator-1 is a human butyrylcholinesterase (BChE) activator and antidote, with a Ki value of 0.52 μM against human BChE. BChE reactivator-1 activates BChE inhibited by organophosphorus compounds, binds reversibly to native BChE, and restores cholinesterase activity in human whole blood. BChE reactivator-1 is applicable to research related to organophosphorus poisoning.
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- CAS No.: 1482498-53-2
- Formule: C18H18BrN3O
- Masse moléculaire:372.26
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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BChE 0.52 μM (Ki) |
BChE reactivator-1 (Oxime 3) (0.1-3000 μM) potently inhibits human BChE with a Ki of 0.52 μM, exhibiting 40-fold higher binding selectivity for BChE than for human AChE[1].
BChE reactivator-1 (100 μM; up to 24 h) is a potent reactivator of human BChE inhibited by cyclosarin, sarin, tabun, VX, and paraoxon, achieving the highest kobs values for cyclosarin- and sarin-inhibited BChE[1].
BChE reactivator-1 (1, 10 μM) enables pseudo-catalytic detoxification of cyclosarin in human whole blood with supplemented BChE, restoring ~60% of total cholinesterase activity within 10 minutes for 30 μM cyclosarin at a 10 μM oxime concentration[1].
BChE reactivator-1 (25-800 μM; 24 h) has an acceptable in vitro safety profile, with no cytotoxicity to human SH-SY5Y and HepG2 cells at concentrations < 100 μM, and IC50 values of ≥ 400 μM (SH-SY5Y) and 248 μM (HepG2)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1482498-53-2
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Masse moléculaire 372.26
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Formule C18H18BrN3O
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SMILES
[H]/C(C1=[N+](C=CN1CC2=CC=CC=C2)CC3=CC=CC=C3)=N/O.[Br-]
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BChE reactivator-1 Related Classifications
HY-183750 Related Classifications
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