产品
编 号：F762947
分子式：C11H13N3
分子量：187.24
分子式：C11H13N3
分子量：187.24
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CAS No: 3026599-90-3
产品详情
生物活性：
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.
体内研究：
JBSNF-000028 (50 mg/kg; p.o.; twice daily for 27 days) improves glucose and lipid handling in mice with diet-induced obesity (DIO).JBSNF-000028 (50 mg/kg; p.o.; twice daily for 4 weeks) improves glucose tolerance in NNMT knockout mice with diet-induced obesity.Animal Model:Male C57BL6/N mice, diet induced obesity (DIO) model
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
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).PK parametersIntravenous Oral
Dose (mg/kg)110
AUC0–t (ng h/mL)4461369
C0/Cmax (ng/mL)432452
Tmax (h)-1.00
T1/2 (h)1.772.36
Tlast (h)8.0010.0
Cl (mL/min/kg)36.6-
Vd (L/kg)8.69-
F (%)-30
体外研究：
JBSNF-000028 (24 h) inhibits NNMT activity with an EC50 of 2.5 μM in U2OS cells.JBSNF-000028 (10-100 μM; 72 h) has no cytotoxicity against HepG2 cells.JBSNF-000028 binds below a hairpin structural motif at the nicotinamide pocket and stacks between Tyr-204 (from Hairpin) and Leu-164 (from central domain).JBSNF-000028 is inactive against a broad panel of targets related to metabolism and safety.
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.
体内研究：
JBSNF-000028 (50 mg/kg; p.o.; twice daily for 27 days) improves glucose and lipid handling in mice with diet-induced obesity (DIO).JBSNF-000028 (50 mg/kg; p.o.; twice daily for 4 weeks) improves glucose tolerance in NNMT knockout mice with diet-induced obesity.Animal Model:Male C57BL6/N mice, diet induced obesity (DIO) model
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
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).PK parametersIntravenous Oral
Dose (mg/kg)110
AUC0–t (ng h/mL)4461369
C0/Cmax (ng/mL)432452
Tmax (h)-1.00
T1/2 (h)1.772.36
Tlast (h)8.0010.0
Cl (mL/min/kg)36.6-
Vd (L/kg)8.69-
F (%)-30
体外研究：
JBSNF-000028 (24 h) inhibits NNMT activity with an EC50 of 2.5 μM in U2OS cells.JBSNF-000028 (10-100 μM; 72 h) has no cytotoxicity against HepG2 cells.JBSNF-000028 binds below a hairpin structural motif at the nicotinamide pocket and stacks between Tyr-204 (from Hairpin) and Leu-164 (from central domain).JBSNF-000028 is inactive against a broad panel of targets related to metabolism and safety.
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