2. Neuronal Signaling Membrane Transporter/Ion Channel PI3K/Akt/mTOR Stem Cell/Wnt Metabolic Enzyme/Protease TGF-beta/Smad
  3. Amyloid-β Cholinesterase (ChE) Calcium Channel GSK-3 Tau Protein Phosphatase Akt PKA
  4. SCR1693

SCR1693 是一种选择性、可逆性、口服活性且非竞争性的乙酰胆碱酯酶 (AChE) 抑制剂 (IC50 = 0.68 μM)，并且是钙通道 (calcium channel) 阻滞剂。SCR1693 能降低 tau 蛋白磷酸化水平，抑制 Aβ 的生成与释放。SCR1693 可修复胰岛素信号通路并改善认知功能障碍。SCR1693 可用于阿尔茨海默病的研究，尤其是伴随 2 型糖尿病的情况。

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SCR1693

SCR1693 Chemical Structure

CAS No. : 1442559-20-7

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SCR1693 相关抗体

Top Publications Citing Use of Products

查看 Cholinesterase (ChE) 亚型特异性产品:

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AChE BChE

查看 Calcium Channel 亚型特异性产品:

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

查看 GSK-3 亚型特异性产品:

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GSK-3 GSK-3α GSK-3β

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

查看 PKA 亚型特异性产品:

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PKA PKAR PKACα

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SCR1693 is a selective, reversible, orally active and noncompetitive inhibitor of AChE (IC50 = 0.68 μM) as well as a calcium channel blocker. SCR1693 reduces tau phosphorylation levels, and inhibits the generation and release of Aβ. SCR1693 restores insulin signaling and improves cognitive deficits. SCR1693 can be used for the study of Alzheimer's disease, especially which complicated with type 2 diabetes mellitus[1][2][3].

IC50 & Target[1]

AChE

 

体外研究
(In Vitro)

SCR-1693 (0.4-5 μM, 24 h) 降低 HEK293/tau 细胞中总 tau 和磷酸化 tau 水平[1]。
SCR-1693 (0.8-20 μM, 6 h) 在短期处理中诱导 HEK293/tau 细胞 tau 去磷酸化并增加总 tau 水平[1]。
SCR-1693 (0.4-4 μM, 24 h) 抑制 N2a/APP 细胞中 Aβ 的生成和释放[1]。
SCR-1693 (3.3-30 μM, 6 h) 主要通过调节其磷酸酶在 Neuro-2a-tau 细胞中下调 tau 磷酸化[2]。
SCR-1693 (10 μM , 6 h) 在 Neuro-2a-tau 细胞中激活 PKA/Akt 通路、抑制 GSK-3β 并增强PP2A/PP1 活性[2]。
SCR-1693 (10 μM, 6 h) 通过调节 PP1/PP2A 在 Neuro-2a-tau 细胞中降低胰岛素抵抗能力[2]。
SCR-1693 (0.01-10 μM, 30 min) 以浓度依赖性抑制 AChE 活性，IC50 值为 0.68 μM，但不抑制 BuChE 活性[3]。
SCR-1693 (1-100 μM) 以剂量依赖性抑制 KCl 诱发的细胞内 Ca2+ 增加，IC50 值为 28.6 μM[3]。
SCR-1693 (0.004-2.5 μM, 48 h) 抑制 Aβ25-35 (HY-P0128) 诱导的 SH-SY5Y 细胞死亡[3]。

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

SCR1693 相关抗体:

Western Blot Analysis[1]

Cell Line: HEK293/tau cells
Concentration: 0.4, 2, 5 μM
Incubation Time: 24 h
Result: Increased tau dephosphorylation level at Ser198/199/202 sites (Tau 1 epitope) concentration dependently.
Reduced total tau level significantly at 5 μM.

Western Blot Analysis[1]

Cell Line: HEK293/tau cells
Concentration: 0.8, 4, 20 μM
Incubation Time: 6 h
Result: Induced tau dephosphorylation at Ser198/199/202 (Tau-1) sites and increased total tau level (4 μM and 20 μM).

Western Blot Analysis[2]

Cell Line: Neuro-2a-tau cells
Concentration: 3.3, 10, 30 μM
Incubation Time: 6 h
Result: Decreased tau phosphorylation levels at the sites of Ser199/202, Ser202/T205, T212/Ser214, Thr231, Ser262 and Ser356, rather than Ser422,and increased tau dephosphorylation level.
Activated PKA and Akt, and inhibited GSK-3β activation.
Decreased the negatively regulated phosphorylation of PP2AC and PP1 at the site of Tyr307 and Thr320, respectively.
Enhanced PP2A and PP1 activity.
Enlarged insulin signaling, especially p-IRS-1 Tyr632 and p-Akt Ser473.
体内研究
(In Vivo)

SCR-1693 (1-4 mg/kg，灌胃给药，每日一次，持续 20 天) 减轻脑室内注射链脲佐菌素 Streptozotocin (STZ) (HY-13753) 诱导的大鼠认知障碍[2]。
SCR-1693 (3-30 mg/kg，口服给药，给药一次) 以剂量依赖性抑制 Wistar 大鼠脑匀浆 AChE 活性[3]。
SCR-1693 (0.1-1 mg/kg，口服给药，每天一次，持续 12 天) 改善 Aβ25-35 处理的小鼠的空间记忆能力[3]。

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

Animal Model: STZ (3 mg/kg) was administered intracerebroventricularly twice in male wistar rats (220-250 g)[2]
Dosage: 1, 2, 4 mg/kg
Administration: i.g., once daily for 20 days
Result: Shortened STZ-injection induced lengthening of escape latency during the training period.
Showed a significant improvement of behavioral performance in the probe trails test.
Restored the levels of GPAF and PSD-95.
Decreased STZ-induced tau hyperphosphorylation in hippocampus of rats.
Decreased deactivated phosphorylation of PP1 and PP2A in a dose-dependent manner.
Animal Model: A single intracerebroventricular (icv) injection of aggregated Aβ25-35 in mice[3]
Dosage: 0.1, 0.3, 1 mg/kg
Administration: p.o. once daily for 12 days
Result: Improved Aβ25-35-impaired learning and both long-term and short-term memory and its effects were stronger than Donepezil (HY-14566) and Memantine (HY-B0591).
Decreased AChE activity.
Prevented Aβ25-35-induced loss of hippocampal pyramidal cells.
Protected hippocampal synaptic transmission and LTP.
Regulated hippocampal protein phosphorylation in Aβ25–35-treated mice.
分子量

425.95

Formula

C24H28ClN3O2
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

SCR1693 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

SCR16931442559-20-7SCR 1693SCR-1693Amyloid-βCholinesterase (ChE)Calcium ChannelGSK-3Tau ProteinPhosphataseAktPKAβ-amyloid peptideAβAbetaCa2+ channelsCa channelsGlycogen synthase kinase-3Glycogen synthase kinase 3PKBProtein kinase BProtein kinase AAlzheimer's diseasetauAChEtype 2 diabetesNeura-2a-tau cellsHEK293/tau cellsInhibitorinhibitorinhibit

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