3026599-90-3

Name	JBSNF-000028 free base
CAS	3026599-90-3
Molecular Formula	C11H13N3
Molecular Weight	187.24
MOL File	3026599-90-3.mol

Synonyms

JBSNF-000028 free base

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Chemical Properties

Boiling point	283.9±50.0 °C(predicted)
density	1.32±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)
form	Solid
pka	13.83±0.20(predicted)
color	Light yellow to yellow

Hazard Information

Uses

JBSNF-000028 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 can be used for the research of metabolic disorders[1].

in vivo

JBSNF-000028 (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 (50 mg/kg; p.o.; twice daily for 4 weeks) improves glucose tolerance in NNMT knockout mice with diet-induced obesity^[1].

Animal Model:	Male C57BL6/N mice, diet induced obesity (DIO) model^[1]
Dosage:	50 mg/kg
Administration:	Oral administration, b.i.d for 27 days
Result:	Significantly reduced the body weight and fed blood glucose. Reduced 1-methyl-nicotinamide (MNA) levels in visceral WAT and liver. Led to a statistically significant reduction in plasma triglyceride, plasma LDL cholesterol, liver triglyceride and liver total cholesterol.

Animal Model:

Male C57BL6/N mice^[1]

Dosage:

1 mg/kg and 10 mg/kg

Administration:

Intravenous and oral administration (Pharmacokinetic Analysis)

Result:

Pharmacokinetic parameters of JBSNF-0000028 in mice following intravenous (1 mg/kg) and oral administration (10 mg/kg)^[1].

PK parameters	Intravenous	Oral
Dose (mg/kg)	1	10
AUC_0–t (ng h/mL)	446	1369
C₀/C_max (ng/mL)	432	452
T_max (h)	-	1.00
T_1/2 (h)	1.77	2.36
T_last (h)	8.00	10.0
Cl (mL/min/kg)	36.6	-
Vd (L/kg)	8.69	-
F (%)	-	30

References

[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. DOI:10.1038/s41598-022-19634-2

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