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首页-小分子抑制剂&激动剂-Others-Other Targets-JBSNF-000028
JBSNF-000028

Chemical Structure : JBSNF-000028

CAS No.: 3026599-90-3

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JBSNF-000028 (JBSNF000028)

货号: PC-49336Not For Human Use, Lab Use Only.

JBSNF-000028 (JBSNF000028) is a potent, selective, orally bioavailable substrate-analog inhibitor of nicotinamide N-methyltransferase (NNMT) with IC50 of 34 nM, 190 and 210 nM against human, monkey and mouse NNMT, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    JBSNF-000028 (JBSNF000028) is a potent, selective, orally bioavailable substrate-analog inhibitor of nicotinamide N-methyltransferase (NNMT) with IC50 of 34 nM, 190 and 210 nM against human, monkey and mouse NNMT, respectively.
    JBSNF-000028 inhibits endogenous cellular NNMT activity in U2OS cells (24 h treatment) with EC50 of 2.5 uM by LCMS/MS detection.
    JBSNF-000028 shows high selectivity in a panel of diabetes/obesity targets, receptor and ion channel panel, and shows no cytotoxicity in HepG2 cells at 100 uM.
    JBSNF-000028 (50 mg/kg, b.i.d, p.o.) improveed glucose and lipid handling in mice with diet-induced obesity (DIO), demonstrated statistically significant reduction in body weight.
    JBSNF-000028 (50 mg/kg, b.i.d, p.o.) showed statistically significant reduction in MNA levels in in genetic model of insulin resistance (ob/ob), with no reduction in fed blood glucose, insulin and plasma triglycerides, plasma total cholesterol, and plasma LDL cholesterol.

    物理化学性质&存储条件

    分子量 187.246
    分子式 C11H13N3
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    2-methyl-1,2,5,6-tetrahydro-3H-pyrrolo[3,2,1-ij]quinazolin-3-imine

    参考文献

    1. Sven Ruf, et al. Sci Rep. 2022 Sep 14;12(1):15440.

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