ASM-IN-1 

ASM-IN-1 is a potent and orally active acid sphingomyelinase (ASM) inhibitor with an IC₅₀ value of 1.5 µM. ASM-IN-1 reduces lipid plaques in the aortic arch and aorta and reduces plasma ceramide concentration and Ox-LDL levels. ASM-IN-1 shows antiatherosclerotic and anti-inflammatory activity^[1].

ASM-IN-1 (compound 4i) (0-20 µM) did not affect cell growth in HUVECs^[1].
ASM-IN-1 (0, 1, 5 µM) reduces the expressions of IL-6 and TNF-α with LPS stimulated in a dose-dependent manner, decreases the expression of MCP-1 mRNA in HUVECs^[1].
ASM-IN-1 (5 µM) reduces Ox-LDL-stimulated MCP-1 mRNA expression and restore IL-6 mRNA to a normal level^[1].

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

ASM-IN-1 (1 mg/kg for i.v.; 10 mg/kg for p.o.) shows good pharmacokinetic properties with good oral bioavailability of 35.42% in ICR mice^[1].
ASM-IN-1 (6, 12, 40 mg/kg; i.p.; twice a day for 8 weeks) antiatherosclerotic activity by inhibiting ASM in mice^[1].
Pharmacokinetic Parameters of ASM-IN-1 in ICR mice^[1].

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

390.19

C₁₆H₁₂BrN₃O₄

BrC1=CC=C(OCC2=CC=C(C3=NOC(C(NO)=O)=N3)C=C2)C=C1

Room temperature in continental US; may vary elsewhere.

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

• [1]. Yang K, et al. Discovery of Novel N-Hydroxy-1,2,4-oxadiazole-5-formamides as ASM Direct Inhibitors for the Treatment of Atherosclerosis. J Med Chem. 2023 Feb 23;66(4):2681-2698.  [Content Brief]