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ZT-1a 

Cat. No.: HY-136532
Handling Instructions

ZT-1a is a potent, non-ATP-competitive and selective SPAK inhibitor. ZT-1a inhibits SPAK activity with IC50s of 44.3, 35.0, 46.7 μM at ATP concentrations of 0.01, 0.1 and 1 mM, respectively.

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ZT-1a Chemical Structure

ZT-1a Chemical Structure

CAS No. : 212135-62-1

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Description

ZT-1a is a potent, non-ATP-competitive and selective SPAK inhibitor. ZT-1a inhibits SPAK activity with IC50s of 44.3, 35.0, 46.7 μM at ATP concentrations of 0.01, 0.1 and 1 mM, respectively[1].

IC50 & Target

SPAK[1]

In Vitro

ZT-1a inhibits Na-K-2Cl cotransporter (NKCC1) and stimulates K-Cl cotransporters (KCCs) by decreasing their SPS1-related proline/alanine-rich kinase (SPAK)-dependent phosphorylation[1].
ZT-1a inhibits phosphorylation of NKCC1 p-Thr203/207/212 by 72±5.2% at 1 µM ZT-1a and phosphorylation of KCC sites 1/2 by 65-77% at 3 µM in HEK-293 cells[1].
SPAK phosphorylation at Ser373 is inhibited by 70±3.8% inhibition at 3-10 µM ZT-1a[1].
ZT-1a (10 µM) inhibits NKCC1 but stimulates KCC3 activity[1].

In Vivo

ZT-1a (10-100 mg/kg) inhibits SPAK-dependent cation-Cl− cotransporters (CCC) phosphorylation in vivo[1].

Animal Model: Naive mice[1]
Dosage: 10, 30, 50, and 100 mg/kg
Administration: Intraperitoneal (i.p.) administration
Result: Inhibited SPAK-dependent cation-Cl- cotransporters (CCC) phosphorylation in vivo.
Molecular Weight

445.73

Formula

C₂₂H₁₅Cl₃N₂O₂

CAS No.

212135-62-1

SMILES

O=C(NC1=CC(Cl)=C(C(C2=CC=C(Cl)C=C2)C#N)C=C1C)C3=CC(Cl)=CC=C3O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

ZT-1aOthersneurologicalSPAKParkinsonInhibitorinhibitorinhibit

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