PeptideDB

JBSNF-000028 hydrochloride

CAS: F: C11H14ClN3 W: 223.70

JBSNF-000028 hydrochloride is an orally active nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 0.033 μM
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This product is for research use only, not for human use. We do not sell to patients.

Bioactivity JBSNF-000028 hydrochloride is an orally active nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 0.033 μM, 0.19 μM and 0.21 μM against human NNMT (hNNMT), monkey NNMT (mkNNMT), and mouse NNMT (mNNMT), respectively. JBSNF-000028 hydrochloride can be used for the research of metabolic disorders[1].
Target IC50: 0.033 μM (hNNMT), 0.19 μM (mkNNMT), 0.21 μM (mNNMT)
Invitro JBSNF-000028 hydrochloride (24 h) inhibits NNMT activity with an EC50 of 2.5 μM in U2OS cells[1].JBSNF-000028 hydrochloride (10-100 μM; 72 h) has no cytotoxicity against HepG2 cells[1].JBSNF-000028 hydrochloride binds below a hairpin structural motif at the nicotinamide pocket and stacks between Tyr-204 (from Hairpin) and Leu-164 (from central domain)[1].JBSNF-000028 hydrochloride is inactive against a broad panel of targets related to metabolism and safety[1].
In Vivo JBSNF-000028 hydrochloride (50 mg/kg; p.o.; twice daily for 27 days) improves glucose and lipid handling in mice with diet-induced obesity (DIO)[1].JBSNF-000028 hydrochloride (50 mg/kg; p.o.; twice daily for 4 weeks) improves glucose tolerance in NNMT knockout mice with diet-induced obesity[1].
Name JBSNF-000028 hydrochloride
Formula C11H14ClN3
Molar Mass 223.70
Transport Room temperature in continental US; may vary elsewhere.
Storage

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

Reference [1]. Ruf S, et al. Novel tricyclic small molecule inhibitors of Nicotinamide N-methyltransferase for the treatment of metabolic disorders. Sci Rep. 2022 Sep 14;12(1):15440.