Anethole trithione derivative-1
Anethole trithione derivative-1 is a derivative of Anethole trithione (HY-B1223), and also a regulator of sulfide:quinone oxidoreductase (SQR) and uncoupling protein 2 (UCP2), with mitochondrial uncoupling-inducing activity and neuroprotective activity. Anethole trithione derivative-1 mediates mitochondrial uncoupling via SQR-dependent reverse electron transport of complex I, ROS-dependent UCP2 activation, and reduction of mitochondrial membrane potential. Anethole trithione derivative-1 reduces brain damage and improves function in mouse models of ischemic and hemorrhagic stroke. Anethole trithione derivative-1 can be used in stroke research.
For research use only. We do not sell to patients.
- Formula: C13H11BrO2S3
- Molecular Weight:375.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
IL-1β |
IL-6 |
TNF-α |
In Vitro
Anethole trithione derivative-1 (compound 16) (1 μM) potently reduces mitochondrial membrane potential in BV2 microglial cells via complex I RET-dependent UCP2 activation, exhibiting strong mitochondrial uncoupling activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male mice (8-12 weeks old, 22-26 g, specific pathogen-free conditions, photothrombotic cerebral ischemia model)[1]
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Dosage:50 mg/kg
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Administration:i.p.; daily; 3 days
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Result:Significantly reduced cerebral infarct volume compared to vehicle-treated controls.
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Animal Model:Male mice (8-12 weeks old, 22-26 g, specific pathogen-free conditions, intracerebral hemorrhage model)[1]
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Dosage:50 mg/kg
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Administration:i.p.; daily; 3 days
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Result:Significantly decreased neuroscores compared to vehicle-treated controls.
Reduced left turn rate compared to vehicle-treated controls.
Increased right paw placement rate compared to vehicle-treated controls.
Reduced water content in the ipsilateral striatum to alleviate brain edema.
Significantly decreased protein levels of proinflammatory factors IL-1β, IL-6, and TNF-α in the ipsilateral striatum.
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Animal Model:Male microglia/macrophage-specific SQR knockout (Cx3cr1Cre:Sqrfl/fl) mice and littermate control Sqrfl/fl mice (8-12 weeks old, 22-26 g, specific pathogen-free conditions, intracerebral hemorrhage model)[1]
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Dosage:50 mg/kg
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Administration:i.p.; daily; 3 days
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Result:Significantly reduced ipsilateral striatal water content relative to vehicle‑treated controls in Sqrfl/fl mice.
Improved neurological function metrics including neuroscores, left‑turn bias and right forelimb placement accuracy relative to vehicle‑treated controls in Sqrfl/fl mice.
Completely abolished all efficacy‑related effects in Cx3cr1Cre:Sqrfl/fl mice, with no significant differences observed between vehicle‑ and compound 16‑treated knockout mice.
Chemical Information
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Molecular Weight 375.32
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Formula C13H11BrO2S3
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SMILES
COC(CCC1=C(SSC1=S)C2=CC=C(C=C2)Br)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- Anethole trithione derivative-1
- Anethole trithione derivative1
- Anethole trithione derivative 1
- Drug Derivative
- Mitochondrial Metabolism
- Interleukin Related
- TNF Receptor
- SQR
- photothrombotic ischemic stroke
- mouse models of hemorrhagic stroke
- Cx3cr1Cre:Sqrfl/fl knockout mice
- BV2 microglial cells
- mouse models of ischemic stroke
- uncoupling protein 2
- sulfide-quinone oxidoreductase
- intracerebral hemorrhage
- UCP2
- Inhibitor
- inhibitor
- inhibit