1. Anti-infection
  2. Influenza Virus
  3. Neuraminidase-IN-11

Neuraminidase-IN-11 (15e) 是一种有效的选择性神经氨酸酶 (NA) 抑制剂,作用于 H1N1、H5N1 和 H5N8 病毒的 NA IC50 值分别是 4.7 nM、8.46 nM、1.5 nM。

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Neuraminidase-IN-11 Chemical Structure

Neuraminidase-IN-11 Chemical Structure

CAS No. : 2685786-28-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Neuraminidase-IN-11 (15e) is a potent and selective neuraminidase (NA) inhibitor with the IC50 values of 4.7 nM, 8.46 nM and 1.5 nM against H1N1, H5N1 and H5N8 NAs respectively[1].

体外研究
(In Vitro)

Neuraminidase-IN-11 (15e) (0-6 μM, 40 min)has anti-NA (Neuraminidase) activity against H1N1-H274Y mutant and H5N1-H274Y mutant with the IC50 values of 1.07 μM and 0.61 μM, respectively[1].
Neuraminidase-IN-11 (15e) (0-20 μM, 48 h) inhibits chicken embryo fibroblasts (CEFs) infected H5N1 or H5N8 with the IC50 values of 4.4 μM and 0.57 μM respectively, and inhibits Madin−Darby canine kidney (MDCK) cells infected H1N1 or H3N2 with the IC50 values of 0.05 μM and 12.65 μM respectively[1].
Neuraminidase-IN-11 (15e) has no significant inhibitory effect on the major CYP enzymes which acts on CYP1A2, CYP2C9 and CYP2C19 with the IC50 values of 28.9 μM, 47.3 μM and 47.8 μM, respectively[1].
The metabolic stability parameters of Neuraminidase-IN-11 (15e) in human liver microsomes (HLM)[1].

Parameters Neuraminidase-IN-11 (15e)
t1/2 (min) >145
CLint(mic) (μL/min/kg) <9.6
CLint(liver) (mL/min/kg) <8.6
remaining (T = 60 min) (%) 79.3

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

体内研究
(In Vivo)

Neuraminidase-IN-11 (15e) (oral administration, 50 mg/kg, every second day, 14 days) shows no significant change in body weight and no other toxic side effects in kunming mice[1].

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

Animal Model: Male Sprague−Dawley rat[1]
Dosage:
Administration: 2 mg/kg, i.v.; 20 mg/kg, p.o.
Result: The pharmacokinetic parameters of Neuraminidase-IN-11 (15e)
Parameters 15e (i.v.) 15e (p.o.)
t1/2 (h) 0.213 0.863
Tmax (h) 0.083 0.5
Cmax (ng/mL) 7195 491
Vdss (mL/kg) 179 -
CL 17.2 -
F (%) - 1.58
分子量

486.62

Formula

C26H34N2O5S

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

Neuraminidase-IN-11 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

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Neuraminidase-IN-11
目录号:
HY-151104
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