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  4. XEN445

XEN445是內(nèi)皮脂肪酶(EL)抑制劑，IC50為0.237 uM，具有很好的ADME和PK活性，能提高小鼠血漿中高密度脂蛋白膽固醇濃度。

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XEN445 Chemical Structure

XEN445 Chemical Structure

CAS No. : 1515856-92-4

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規(guī)格 價(jià)格 是否有貨 數(shù)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   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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.

細(xì)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 號(hào)
性狀

固體

顏色

Light brown to brown

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 40 mg/mL (109.19 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.85%

參考文獻(xiàn)

XEN445 相關(guān)分類(lèi)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱(chēng)：
XEN445
目錄號(hào)：
HY-12246
需求量：