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 exhibits the highest activity in binding to ASM, with an IC₅₀ value of 0.87 μM^[1].
ASM-IN-2 exhibits weak cytotoxicity at a high concentration of 100 μM in the experiment testing the anti-proliferative effects on human neuroblastoma cells SH-SY5Y using CCK8 (the cell survival rates are higher than 78%)^[1].

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

ASM-IN-2 (1 or 10 MG/KG, iv or ip) is rapidly absorbed (Tmax = 0.25 h) in male ICR mice with a high maximum concentration (Cmax = 4204.13 NG/ML) and moderate bioavailability (F=39.59%), which possesses an acceptable profile for antidepressant studies^[1].
ASM-IN-2 (6, 12, 24 MG/KG, i.p., 10 days) significantly reduces the immobility time of mice better than fluoxetine(12 mg/kg) (HY-W011235) in the forced swim test (FST) and tail suspension test (TST). ASM-IN-2 results in a significant increase in the expression of BDNF and increases the level of ceramide in the hippocampal and cerebral cortex. ASM-IN-2 improves the levels of oxidative stress in the brains of depressed mice through inhibiting ASM activity^[1].
ASM-IN-2 (6, 12, 24 MG/KG, i.p.) reduces the levels of TNF-α, IL-1β and IL-6 in a dose-dependent manner in CUMS model mice, attenuating the inflammatory response in the serum of mice^[1].
ASM-IN-2 (6, 12, 24 MG/KG, i.p.) significantly increases the levels of 5-HT in the hippocampus of mice, thereby promoting more effective antidepressant activity by inhibiting ASM^[1].

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

392.63

C₁₆H₁₁BrClN₃O₂

2305789-66-4

O=C(C1=NN(C(C2=CC=C(C=C2)Br)=C1)C3=CC=C(C=C3)Cl)NO

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• [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]