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  4. XEN445

XEN445是内皮脂肪酶(EL)抑制剂，IC50为0.237 uM，具有很好的ADME和PK活性，能提高小鼠血浆中高密度脂蛋白胆固醇浓度。

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XEN445 Chemical Structure

XEN445 Chemical Structure

CAS No. : 1515856-92-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥476
In-stock
5 mg ￥433
In-stock
10 mg ￥718
In-stock
25 mg ￥1507
In-stock
50 mg ￥2335
In-stock
100 mg ￥3502
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

XEN445 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

XEN445 is a potent and selective EL inhibitor(IC50=0.237 uM), that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice. IC50 value: 0.237 uM [1] Target: Endothelial lipase inhibitor XEN445 can be readily prepared in good yield from commercial available chemicals, which was selected for further evaluation of this series of EL inhibitors. After a 30 min preincubation of EL-expressing HEK cells with XEN445, the IC50 value for XEN445 of 0.25 lM was obtained. This value was very similar to that determined in the cell-free assay. Wild-type mice were orally dosed with XEN445 at 30 mg/kg b.i.d. for 3 days and blood was taken on the morning of day 4, 16 h post final dose. At termination, the average plasma levels of XEN445 was 9.9 lM and the drug caused an 18% and 16% increase in total plasma cholesterol and HDLc, respectively.

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
0.25 μM
Compound: 13, XEN445
Inhibition of full length human endothelial lipase transfected in HEK293 cells using PED-A1 as substrate preincubated for 30 mins followed by substrate addition by fluorescence assay
Inhibition of full length human endothelial lipase transfected in HEK293 cells using PED-A1 as substrate preincubated for 30 mins followed by substrate addition by fluorescence assay
[PMID: 24211162]
分子量

366.33

Formula

C18H17F3N2O3
CAS 号
性状

固体

颜色

Light brown to brown

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 40 mg/mL (109.19 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7298 mL 13.6489 mL 27.2978 mL
5 mM 0.5460 mL 2.7298 mL 5.4596 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.85%

COA (285 KB) HNMR (239 KB) LCMS (93 KB)

产品使用指南 (1538 KB)
参考文献

XEN445 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7298 mL 13.6489 mL 27.2978 mL 68.2445 mL
5 mM 0.5460 mL 2.7298 mL 5.4596 mL 13.6489 mL
10 mM 0.2730 mL 1.3649 mL 2.7298 mL 6.8244 mL
15 mM 0.1820 mL 0.9099 mL 1.8199 mL 4.5496 mL
20 mM 0.1365 mL 0.6824 mL 1.3649 mL 3.4122 mL
25 mM 0.1092 mL 0.5460 mL 1.0919 mL 2.7298 mL
30 mM 0.0910 mL 0.4550 mL 0.9099 mL 2.2748 mL
40 mM 0.0682 mL 0.3412 mL 0.6824 mL 1.7061 mL
50 mM 0.0546 mL 0.2730 mL 0.5460 mL 1.3649 mL
60 mM 0.0455 mL 0.2275 mL 0.4550 mL 1.1374 mL
80 mM 0.0341 mL 0.1706 mL 0.3412 mL 0.8531 mL
100 mM 0.0273 mL 0.1365 mL 0.2730 mL 0.6824 mL
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:

XEN4451515856-92-4XEN 445XEN-445OthersInhibitorinhibitorinhibit

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产品名称：
XEN445
目录号：
HY-12246
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