产品
编 号：F757094
分子式：C9H11N3O
分子量：177.2
分子式：C9H11N3O
分子量：177.2
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CAS No: 2947393-64-6
产品详情
生物活性：
NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC50 values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT.
体内研究：
1.19Pharmacokinetic Properties of NNMT-IN-4 in Mice. MicePO 50 mg/kg
T1/2 (h)2.89
Tmax (h)0.250
Cmax (ng/mL)22500
AUClast (ng*h/mL)51115
CI (1 mg/kg IV) (mL/min/kg)36.1
F (%)220
体外研究：
NNMT-IN-4 (5 nM-0.5 mM; 24 h) shows inhibitory effect to NNMT with an IC50 value of 38 nM in K562 cells.NNMT-IN-4 (5 nM-0.5 mM; 24 h) shows inhibitory effect to NNMT with an IC50 value of 42 nM in promega MTase-Glo methyltransferase assay.
NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC50 values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT.
体内研究：
1.19Pharmacokinetic Properties of NNMT-IN-4 in Mice. MicePO 50 mg/kg
T1/2 (h)2.89
Tmax (h)0.250
Cmax (ng/mL)22500
AUClast (ng*h/mL)51115
CI (1 mg/kg IV) (mL/min/kg)36.1
F (%)220
体外研究：
NNMT-IN-4 (5 nM-0.5 mM; 24 h) shows inhibitory effect to NNMT with an IC50 value of 38 nM in K562 cells.NNMT-IN-4 (5 nM-0.5 mM; 24 h) shows inhibitory effect to NNMT with an IC50 value of 42 nM in promega MTase-Glo methyltransferase assay.
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