1. Neuronal Signaling
  2. Cholinesterase (ChE)
  3. Trimedoxime dichloride

Trimedoxime dichloride  (Synonyms: TMB-4 dichloride)

Cat. No.: HY-165600
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Trimedoxime dichloride (TMB-4 dichloride) is a blood-brain barrier-permeable cholinesterase reactivator. Trimedoxime dichloride reactivates cholinesterase inhibited by paraoxon, sarin, tabun and other agents, restricts the breakdown of acetylcholine and alleviates excessive cholinergic stimulation. Trimedoxime dichloride reduces mortality and prolongs survival time. Trimedoxime dichloride exhibits reactivation efficacy against AChE in rat tissues. Trimedoxime dichloride can be used in research related to organophosphate (paraoxon) poisoning and tabun poisoning.

For research use only. We do not sell to patients.

Trimedoxime dichloride

Trimedoxime dichloride Chemical Structure

CAS No. : 3613-82-9

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Description

Trimedoxime dichloride (TMB-4 dichloride) is a blood-brain barrier-permeable cholinesterase reactivator. Trimedoxime dichloride reactivates cholinesterase inhibited by paraoxon, sarin, tabun and other agents, restricts the breakdown of acetylcholine and alleviates excessive cholinergic stimulation. Trimedoxime dichloride reduces mortality and prolongs survival time. Trimedoxime dichloride exhibits reactivation efficacy against AChE in rat tissues. Trimedoxime dichloride can be used in research related to organophosphate (paraoxon) poisoning and tabun poisoning[1][2][3].

IC50 & Target[1]

AChE

 

Parmacokinetics
Species Dose Route T1/2α T1/2β AUC0-∞ CLtotal Vd V1
Mice[2] 55.98 μM/kg i.v. 8.96 min 108.08 min 74.5867 μM/L·h 0.0125 L/min/kg 1.95 L/kg 0.22 L/kg
In Vivo

Trimedoxime (25 µM per rat; i.p.; single administration) dichloride exerts a protective effect against paraoxon-induced death in male Wistar rats[1].
Trimedoxime (7.5 mg/kg; i.m.; single dose) dichloride significantly reactivates acetylcholinesterase (AChE) inhibited by tabun in rat blood and diaphragm, with reactivation rates of 17.5% and 34.7%, respectively, but exerts extremely weak reactivation on this enzyme in rat brain (only 2.8%), and reduces the acute lethal effect of tabun in mice[3].

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

Animal Model: Wistar (male, 200-250 g, organophosphate poisoning model via intraperitoneal paraoxon exposure)[1]
Dosage: 25 µM/rat
Administration: i.p.; single dose
Result: Reduced 48-hour mortality to 38% in rats exposed to 1 µmol/rat paraoxon.
Reduced 48-hour mortality to 76% in rats exposed to 10 µmol/rat paraoxon.
Reduced 48-hour mortality to 83% in rats exposed to 15 µmol/rat paraoxon.
Lowered the relative risk of death to 0.36 (95% confidence interval, 0.26 to 0.50) compared to paraoxon-only controls.
Animal Model: Wistar (male, 180-200 g, tabun poisoning model)[3]
Dosage: 7.5 mg/kg
Administration: i.m.; single prophylactic dose
Result: Produced 17.5% reactivation of tabun-inhibited AChE in blood.
Produced 34.7% reactivation of tabun-inhibited AChE in diaphragm.
Produced 2.8% reactivation of tabun-inhibited AChE in brain.
Showed significant differences from atropine-only control and HI-6 treatment group.
Increased the LD50 of tabun in mice to 504.8 μg/kg.
Resulted in a protective ratio of 1.71.
Showed significant difference from untreated group and HI-6 treatment group.
Molecular Weight

357.24

Formula

C15H18Cl2N4O2

CAS No.
SMILES

O/N=C/C1=CC=[N+](CCC[N+]2=CC=C(C=C2)/C=N/O)C=C1.[Cl-].[Cl-]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Trimedoxime dichloride Related Classifications

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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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Trimedoxime dichloride
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HY-165600
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