2. Metabolic Enzyme/Protease Neuronal Signaling
  3. SGK Tau Protein
  4. SGK1-IN-7

SGK1-IN-7 是一种可穿过血脑屏障的 SGK1 抑制剂，其 IC50 为 0.72 μM。SGK1-IN-7 可降低 Ser396 和 Ser214 表位上的 TAU 蛋白磷酸化水平。SGK1-IN-7 对 Okadaic acid (HY-N6785) 诱导的毒性具有拮抗作用。SGK1-IN-7 可用于阿尔茨海默病的研究。

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SGK1-IN-7

SGK1-IN-7 Chemical Structure

CAS No. : 3109982-58-0

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SGK1-IN-7 相关抗体

Top Publications Citing Use of Products

查看 SGK 亚型特异性产品:

查看所有亚型
SGK1 SGK3 SGK2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SGK1-IN-7 is a blood-brain barrier-permeable SGK1 inhibitor with an IC50 of 0.72 μM. SGK1-IN-7 reduces the phosphorylation level of TAU protein at the Ser396 and Ser214 epitopes. SGK1-IN-7 antagonizes the toxicity induced by Okadaic acid (HY-N6785). SGK1-IN-7 can be used in the research of Alzheimer's disease[1].

体外研究
(In Vitro)

SGK1-IN-7 (Compound 102) (6.25-50 μM; 30 min) 无致突变性且心脏安全风险低，对 hERG 或 Nav1.5 通道无显著抑制作用，对 Cav1.2 通道仅存在中度抑制 (IC50 = 12.1 μM)[1]。
SGK1-IN-7 (5 μM; 24 h) 在 5 μM 浓度下对经 Okadaic acid 处理的人神经母细胞瘤 SH-SY5Y 细胞发挥显著的神经保护作用[1]。
SGK1-IN-7 (5 μM; 24 h) 可在 5 μM 浓度下显著降低 SH-SY5Y 人神经母细胞瘤细胞中 tau 蛋白在 Ser396 和 Ser214 位点的磷酸化水平，且不改变总 tau 蛋白的表达量[1]。

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

SGK1-IN-7 相关抗体:

Cell Viability Assay[1]

Cell Line: SH-SY5Y human neuroblastoma cells
Concentration: 5 μM
Incubation Time: 24 h (OA pre-treatment)
Result: Significantly restored cell viability in OA-treated SH-SY5Y cells, showing a statistically significant neuroprotective effect compared to OA-only treatment.
药代动力学
(Parmacokinetics)
Species Dose Route Tmax (Plasma) AUClast T1/2 Bioavailability
Mice[1] 2.5 mg/kg i.v. / 954.87 ng·h/mL 0.93 h /
Mice[1] 5 mg/kg i.p. 0.25 h 793.15 1.24 h /
Mice[1] 10 mg/kg p.o. 0.50 h 806.97 ng·h/mL 1.83 h 21 %
体内研究
(In Vivo)

SGK1-IN-7 (Compound 102) (2.5-10 mg/kg；静脉注射、腹腔注射、口服；单次给药) 在雄性 BALB/c 小鼠中表现出剂量依赖性的血浆和脑暴露水平，静脉注射、腹腔注射和口服单次给药后的脑-血浆比 (brain-Kp) 分别为 0.49、0.18 和 0.25[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

385.25

Formula

C19H14Cl2N4O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SGK1-IN-7 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SGK1-IN-73109982-58-0SGKTau ProteinSerum-glucocorticoid regulated kinaseSerum and glucocorticoid-regulated kinaseSH-SY5Y human neuroblastoma cellsRSK2TAU proteinROCK2CLK2MSK1alzheimer's diseaseSGK1miceERK family membersInhibitorinhibitorinhibit

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