ASM-IN-2 

ASM-IN-2 (Compound 46) is a potent ASM inhibitor with an IC₅₀ value of 0.87 μM, displaying good drug-like properties. ASM-IN-2 involves in multiple antidepressant mechanisms of actionin, which are associated with a decline of ceramide. It demostrates remarkable antidepressant effects in the CUMS-induced mouse, which is promising for research in the field of antidepressant drugs^[1].

ASM-IN-2 对 ASM 的结合中表现出最高活性，IC₅₀ 值为 0.87 μM^[1]。
ASM-IN-2 在用 CCK8 检测对人神经母细胞瘤细胞 SH-SY5Y 的抗增殖作用实验中，较高浓度100 μM 时表现出轻微细胞毒性（细胞存活率高于78%）^[1]。

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

ASM-IN-2 (1或10 MG/KG, i.v. 或i.p.) 在雄性 ICR 鼠中被迅速吸收(Tmax = 0.25 h)，达到较高的最大浓度 (Cmax = 4204.13 NG/ML) 和适中的生物利用度 (F = 39.59%)， 适用于抗抑郁药的研究^[1]。
ASM-IN-2 (6, 12, 24 MG/KG, i.p., 10天) 在强迫游泳测试 (FST) 和尾悬试验 (TST) 中显著减少了小鼠不动时间，效果优于氟西汀(12 MG/KG) (HY-W011235)。ASM-IN-2 显著增加 BDNF 表达和大脑皮层中神经鞘脂类物质 ceramide 水平，还通过抑制 AMS 活性改善了氧化应激水平^[1]。
ASM-IN-2 (6, 12, 24 MG/KG, i.p.) 在 CUMS 小鼠模型中以剂量依赖性的方式降低 TNF-α, IL-1β和IL-6的水平，减弱小鼠血清中的炎症反应^[1]。
ASM-IN-2 (6, 12, 24 MG/KG, i.p.) 明显增加小鼠海马组织中 5-HT 的含量，从而通过抑制 ASM 促进更有效的抗抑郁活性^[1]。

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

392.63

C₁₆H₁₁BrClN₃O₂

2305789-66-4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Shi S, et al. Discovery of a Novel ASM Direct Inhibitor with a 1,5-Diphenyl-pyrazole Scaffold and Its Antidepressant Mechanism of Action[J]. J Med Chem. 2024 Jun 18:1520-4804.  [Content Brief]