212135-62-1
中文名稱
ZT-1A
英文名稱
Benzamide, 5-chloro-N-[5-chloro-4-[(4-chlorophenyl)cyanomethyl]-2-methylphenyl]-2-hydroxy-
CAS
212135-62-1
分子式
C22H15Cl3N2O2
分子量
445.73
MOL 文件
212135-62-1.mol
更新日期
2024/07/23 09:31:03
212135-62-1 結(jié)構(gòu)式
基本信息
英文別名
ZT-1aBenzamide, 5-chloro-N-[5-chloro-4-[(4-chlorophenyl)cyanomethyl]-2-methylphenyl]-2-hydroxy-
物理化學(xué)性質(zhì)
沸點538.7±50.0 °C(Predicted)
密度1.442±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO: 125 mg/mL (280.44 mM)
酸度系數(shù)(pKa)7?+-.0.43(Predicted)
形態(tài)Solid
顏色White to off-white
常見問題列表
生物活性
ZT-1a 是一種有效的非 ATP 競爭性的選擇性 SPAK 抑制劑。ZT-1a 抑制 SPAK 活性，在 ATP 濃度為 0.01、0.1 和 1 mM 時，IC50 分別為 44.3、35.0、46.7 μM。靶點
SPAK
體外研究
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.
體內(nèi)研究
ZT-1a (10-100?mg/kg) inhibits SPAK-dependent cation-Cl? cotransporters (CCC) phosphorylation in vivo.
| 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. |