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,适用于对基线干扰要求严格的色谱和分析工作流程。
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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
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