NNMT-IN-8 

NNMT-IN-8 is a non-SAM-mimicking bisubstrate inhibitor and a selective methyltransferase NNMT inhibitor, with IC₅₀ values of 0.0084 μM and 0.0085 μM against human NNMT, and an IC₅₀ of 0.0072 μM against mouse NNMT. NNMT-IN-8 exhibits prominent renal distribution characteristics and moderate bioavailability in rodents. NNMT-IN-8 dose-dependently inhibits renal NNMT in renal fibrosis models, thereby exerting antifibrotic effects. NNMT-IN-8 can be used to investigate the mechanisms of renal fibrosis^[1].

NNMT-IN-8 (compound 16) inhibits NNMT activity in cells overexpressing human NNMT, with an IC₅₀ of 0.25 μM^[1].
NNMT-IN-8 exhibits metabolic stability in human liver microsomes, rat liver microsomes, and mouse liver microsomes, with 79%, 34%, and 23% remaining after 30 min of incubation^[1].
NNMT-IN-8 (3 μM) inhibits hERG current by 15%, indicating a low risk of cardiotoxicity^[1].

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

In rat pharmacokinetic studies, NNMT-IN-8 (compound 16) exhibits moderate total clearance (C_Ltot=32 mL/min/kg), a half-life (t_1/2) of 1.7 h, a maximum plasma concentration (C_max) of 38 nM, and a relatively high serum free fraction (f_u= 30%/20%). NNMT-IN-8 also shows significant renal distribution with a kidney/plasma partition coefficient of 16, as well as moderate oral bioavailability (F=26%)^[1].

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

440.53

C₂₃H₂₅FN₄O₂S

3124204-81-2

O=C1SC2=C(NCC34CCC(CC3)(C4)NCC5=C(F)C(C(N)=O)=CC=C5)C=CC=C2N1

Room temperature in continental US; may vary elsewhere.

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

• [1]. Yoshida S, et al. Structure-Based Drug Discovery of Non-SAM-Mimetic Bisubstrate Inhibitors against Nicotinamide N-Methyltransferase[J]. ACS Medicinal Chemistry Letters, 2026.