1. Metabolic Enzyme/Protease
  2. Phospholipase
  3. ASM-IN-3

ASM-IN-3 (Compound 21b) 是一个具有选择性和血脑屏障穿透性的 acid sphingomyelinase (ASM) 抑制剂 (对纯化的人 ASM 的 IC50 为 3.37 μM)。ASM-IN-3 通过抑制海马中 ASM 活性和增加神经发生,改善 Reserpine (HY-N0480) 诱导的抑郁大鼠抑郁样行为。

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ASM-IN-3 Chemical Structure

ASM-IN-3 Chemical Structure

CAS No. : 2342576-75-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ASM-IN-3 (Compound 21b) is a selective and BBB-penetrating acid sphingomyelinase (ASM) inhibitor (IC50: 3.37 μM for pure human ASM). ASM-IN-3 improves depression-like behaviors by inhibiting ASM activity and increasing neurogenesis in hippocampus in Reserpine (HY-N0480)-induced depressed rats[1].

体外研究
(In Vitro)

ASM-IN-3 (40 μM, 0.5-4 h) 可有效穿透 hCMEC/D3 细胞膜[1]
ASM-IN-3 (0.098-12.5 μM) 对 NIH3T3 细胞是安全的 (IC50: 161 μM)[1]

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

体内研究
(In Vivo)

ASM-IN-3 (48 mg/kg,腹腔注射) 能很好地穿透 SD 大鼠血脑屏障,因为其在脑组织中的含量远高于血浆中的含量[1]
ASM-IN-3 (6-24 mg/kg,静脉注射,每天两次,连续 2 周) 通过降低海马中 ASM 活性和恢复神经发生,在 Reserpine (HY-N0480) 诱导的抑郁大鼠中显示出良好的抗抑郁样作用[1]

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

Animal Model: Reserpine-induced depressed SD rats (6−8 weeks, 200 g, female, were injected intraperitoneally with Reserpine (4 mg/kg) daily)[1]
Dosage: 6, 12, 24 mg/kg
Administration: Intraperitoneal injection (i.p.), twice a day for 2 weeks
Result: Improved sugar consumption in a dose dependent manner after 2 days of tap water drinking and following 20 h of water depletion and fasting.
Decreased the total time in center of rats, and increased times passing the grid and frequency of grooming in the open-field test.
Demonstrated a reduction of the cortical and hippocampal ASM activity by approximately 27% and 33%, respectively, compared to the model group at a dose of 24 mg/kg.
Prevented the inhibitory effect of Reserpine on neurogenesis and restored neurogenesis.
分子量

344.75

Formula

C17H13ClN2O4

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
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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.

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产品名称:
ASM-IN-3
目录号:
HY-171033
需求量: