CAII/VII-IN-1
CAII/VII-IN-1 is an orally active hCA II (KI = 12.3 nM), and hCA VII (KI = 22.6 nM) inhibitor, showing no significant activity against hCA I. CAII/VII-IN-1 shows excellent neuroprotective activity in vivo Pilocarpine (HY-B0726A)-induced seizure model. CAII/VII-IN-1 can upregulate KCC2 and inhibit mTOR, exerting neuroprotective effects. CAII/VII-IN-1 does not show any significant neurotoxic effects or alterations in liver and kidney function. CAII/VII-IN-1 can be used for the study of epilepsy.
For research use only. We do not sell to patients.
- CAS No.: 3085155-69-4
- Formula: C27H23ClN8O5S2
- Molecular Weight:639.11
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Storage:
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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
CAII/VII-IN-1 (Compound 16d) is safe at the given concentration in Vero cells (IC50 = 59.7 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male mice (20-25 g) were injected with Pilocarpine[1].
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Dosage:200 mg/kg
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Administration:Orally before Pilocarpine injection
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Result:Delayed seizures by more than twice as long as the Pilocarpine group (108.6 %).
Showed comparable efficacy in delaying seizure onset and reducing severity at most time points.
Reached 100 % survival.
Upregulated KCC2 (188.1%) and inhibited mTOR (51.39%) exert neuroprotective effects.
Chemical Information
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CAS No. 3085155-69-4
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Molecular Weight 639.11
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Formula C27H23ClN8O5S2
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SMILES
ClC1=CC=C(C=C1)C2=NN(C=C2/C=N/NC(C3=C(N(N=N3)C4=CC=C(C=C4)S(N)(=O)=O)C)=O)C5=CC=C(C=C5)S(C)(=O)=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.
Protocols
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CAII/VII-IN-1 Related Classifications
HY-178362 Related Classifications
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