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NNMT-IN-4 (compound 38) 是选择性的、非竞争性的以及可透过膜的烟酰胺 N-甲基转移酶 (NNMT) 抑制剂,IC50 值分别为 42 和 38 nM 在体外生化和细胞实验中。NNMT-IN-4 具有良好的 PK/PD 和安全性,以及良好的口服生物利用度和制药性能。NNMT-IN-4 可用作 NNMT 的体内化学探针。

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NNMT-IN-4 Chemical Structure

NNMT-IN-4 Chemical Structure

CAS No. : 2947393-64-6

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1 mg ¥2800
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5 mg ¥7200
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target

IC50: 38 nM (NNMT, in K562 cells), 42 nM (promega MTase-Glo methyltransferase assay)[1]

体外研究
(In Vitro)

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[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

1.19 Pharmacokinetic Properties of NNMT-IN-4 in Mice[1].

Mice
PO 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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

177.20

Formula

C9H11N3O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

NNMT-IN-4 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
NNMT-IN-4
目录号:
HY-151813
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