JBSNF-000088

  Cat. No.:  DC21162   Featured
Chemical Structure
7150-23-4
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More than 5000 active chemicals with high quality for research!
Field of application
JBSNF-000088 (6-Methoxynicotinamide) is a small molecule nicotinamide analog that inhibits Nicotinamide N-methyltransferase (NNMT) with IC50 of 1.8, 2.8 and 5.0?μM for human, monkey and mouse NNMT, respectively.
Cas No.: 7150-23-4
Chemical Name: 6-Methoxynicotinamide
Synonyms: JBSNF000088;6-Methoxynicotinamide
SMILES: COc1ccc(cn1)C(=O)N
Formula: C7H8N2O2
M.Wt: 152.153
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
Description: JBSNF-000088 (6-Methoxynicotinamide), a analog of nicotinamide (NA), is a potent Nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 1.8 µM, 2.8 µM, and 5.0 µM for human NNMT, monkey NNMT and mouse NNMT, respectively. JBSNF-000088 inhibits NNMT activity, reduces MNA levels and drives insulin sensitization, glucose modulation and body weight reduction in animal models of metabolic disease[1].
Target: IC50: 1.8 µM (human NNMT), 2.8 µM (monkey NNMT) and 5.0 µM (mouse NNMT)[1]
In Vivo: JBSNF-000088 (6-Methoxynicotinamide) (50 mg/kg; oral route of administration for four weeks) shows statistically significant reduction in body weight (%) and leads to a statistically significant reduction in fed blood glucose on day 21[1]. JBSNF-000088 (50 mg/kg; oral gavage administration; twice daily for four weeks) leads to a statistically significant improvement in oral glucose tolerance on day 28 with glucose tolerance being normalized[1]. JBSNF-000088 (1 mg/kg; intravenous administration; for 4 hours) results in low plasma clearance of 21 mL/min▪kg and the volume of distribution at steady state of 0.7 L/kg, a very short plasma half-life of 0.5 hours upon intravenous administration[1]. JBSNF-000088 (10 mg/kg; oral gavage; for 4 hours) results in a Cmax of 3568 ng/mL with a Tmax value of 0.5 hours, indicating rapid absorption in the intestine, and half-life of 0.4 hours by oral gavage. The oral bioavailability is found to be approximately 40%[1]. Animal Model: Mice with high fat diet (HFD)-induced obesity[1] Dosage: 50 mg/kg Administration: Oral route of administration for four weeks; oral gavage administration and twice daily for four weeks Result: Showed statistically significant reduction in body weight (%) and led to a statistically significant reduction in fed blood glucose on day 21 by oral route of administration. Led to a statistically significant improvement in oral glucose tolerance on day 28 with glucose tolerance being normalized by oral gavage administration. Animal Model: C57BL/6 mice[1] Dosage: 1 mg/kg (Intravenous administration);10 mg/kg (oral gavage)(Pharmacokinetic Study) Administration: Intravenous administration and oral gavage; for 4 hours Result: Resulted in low plasma clearance of 21 mL/min▪kg and the volume of distribution at steady state of 0.7 L/kg, a very short plasma half-life of 0.5 h upon intravenous administration. Resulted in a Cmax of 3568 ng/mL with a Tmax value of 0.5 hours, indicating rapid absorption in the intestine, and half-life of 0.4 hours by oral gavage.
In Vitro: JBSNF-000088 (6-Methoxynicotinamide) has IC50 values are 1.6 and 6.3 µM for U2OS or differentiated 3T3L1 cells[1].
References: [1]. Kannt A, et al. A small molecule inhibitor of Nicotinamide N-methyltransferase for the treatment of metabolic disorders. Sci Rep. 2018 Feb 26;8(1):3660.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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