1. Metabolic Enzyme/Protease Membrane Transporter/Ion Channel PI3K/Akt/mTOR
  2. Carbonic Anhydrase NKCC mTOR
  3. 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.

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CAII/VII-IN-1

CAII/VII-IN-1 Chemical Structure

CAS No. : 3085155-69-4

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Description

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[1].

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.

In Vivo

CAII/VII-IN-1 (200 mg/kg, oral gavage, once) produces pronounced anti-convulsant and anti-epileptogenic effects in Pilocarpine-induced mice, as manifested by a two-fold increase in seizure onset latency, a substantial reduction in seizure severity, and the restoration of hippocampal homeostasis [1].

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

Animal Model: Adult male mice (20-25 g) were injected with Pilocarpine[1].
Dosage: Orally before Pilocarpine injection.
Administration: Delayed seizures by more than twice as long as the Pilocarpine group (108.6 %).
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.
Molecular Weight

639.11

Formula

C27H23ClN8O5S2

CAS No.
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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Room temperature in continental US; may vary elsewhere.

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

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Product Name:
CAII/VII-IN-1
Cat. No.:
HY-178362
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