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  4. JBSNF-000028 free base

JBSNF-000028 是一种具有口服活性的烟酰胺 N-甲基转移酶 (NNMT) 抑制剂，对人 NNMT (hNNMT)、猴 NNMT (mkNNMT) 和小鼠 NNMT (mNNMT) 的 IC50 分别为 0.033 μM、0.19 μM 和 0.21 μM。

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JBSNF-000028 free base Chemical Structure

JBSNF-000028 free base Chemical Structure

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JBSNF-000028 free base 的其他形式现货产品:

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JBSNF-000028 free base 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target

IC50: 0.033 µM (hNNMT), 0.19 µM (mkNNMT), 0.21 µM (mNNMT)[1]
体外研究
(In Vitro)

JBSNF-000028 (24 h) inhibits NNMT activity with an EC50 of 2.5 µM in U2OS cells[1].
JBSNF-000028 (10-100 μM; 72 h) has no cytotoxicity against HepG2 cells[1].
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)[1].
JBSNF-000028 is inactive against a broad panel of targets related to metabolism and safety[1].

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

JBSNF-000028 free base 相关抗体:
体内研究
(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].

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

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
AUC0–t (ng h/mL) 446 1369
C0/Cmax (ng/mL) 432 452
Tmax (h) - 1.00
T1/2 (h) 1.77 2.36
Tlast (h) 8.00 10.0
Cl (mL/min/kg) 36.6 -
Vd (L/kg) 8.69 -
F (%) - 30
分子量

187.24

Formula

C11H13N3
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

JBSNF-000028 free base 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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.

Keywords:

JBSNF-000028JBSNF000028JBSNF 000028Otherstype 2 diabetesliver diseasesnicotinamide N-methyltransferaseNNMTInhibitorinhibitorinhibit

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产品名称：
JBSNF-000028 free base
目录号：
HY-151500
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