ZT-1a - 10mM in DMSO , CAS No.212135-62-1

CAS: 212135-62-1 Cat. No.: Z654554 Peso molecular: 445.73 PubChem CID: 10789506

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

ZT-1a is a potent, non-ATP-competitive and selective SPAK inhibitor. ZT-1a inhibits SPAK activity with IC 50 s of 44.3, 35.0, 46.7 μM at ATP concentrations of 0.01, 0.1 and 1 mM, respectively

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. 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. SPAK phosphorylation at Ser373 is inhibited by 70±3.8% inhibition at 3-10 µM ZT-1a. ZT-1a (10 µM) inhibits NKCC1 but stimulates KCC3 activity. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

ZT-1a (10-100 mg/kg) inhibits SPAK-dependent cation-Cl− cotransporters (CCC) phosphorylation in vivo . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Naive mice Dosage: 10, 30, 50, and 100 mg/kg Administration: Intraperitoneal (i.p.) administration Result: Inhibited SPAK-dependent cation-Cl - cotransporters (CCC) phosphorylation in vivo.

IC50& Target:SPAK

Specifications

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

ZT-1a is a potent, non-ATP-competitive and selective SPAK inhibitor. ZT-1a inhibits SPAK activity with IC 50 s of 44.3, 35.0, 46.7 μM at ATP concentrations of 0.01, 0.1 and 1 mM, respectively.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Nombres e identificadores

• Isómeros SMILES: CC1=CC(=C(C=C1NC(=O)C2=C(C=CC(=C2)Cl)O)Cl)C(C#N)C3=CC=C(C=C3)Cl
• PubChem CID: 10789506
• Peso molecular: 445.73