2. Membrane Transporter/Ion Channel
  3. P-glycoprotein
  4. Encequidar

Encequidar  (Synonyms: HM30181; HM30181A)

目录号: HY-13646 纯度: ≥98.0%
COA 产品使用指南

摩尔计算器

Encequidar (HM30181; HM30181A) 是一种有效的选择性的P-glycoprotein抑制剂。

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Encequidar Chemical Structure

Encequidar Chemical Structure

CAS No. : 849675-66-7

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规格 价格 是否有货 数量
1 mg ￥545
In-stock
5 mg ￥1200
In-stock
10 mg ￥1800
In-stock
50 mg ￥5400
In-stock
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Customer Review

Other Forms of Encequidar:

Encequidar 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Encequidar (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein.

体外研究
(In Vitro)

Encequidar (HM30181; HM30181A) is shown to be approximately equipotent with the reference Pgp inhibitor tariquidar in inhibiting rhodamine 123 efflux from CCRF-CEM T cells (IC50, tariquidar: 8.2±2.0 nM, Encequidar (HM30181): 13.1±2.3 nM) [1].
Encequidar (HM30181) shows a high selectivity for mP-gp and its potency is 20-50 times higher than that of tariquitar, another third generation P-gp inhibitor[2].

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

Encequidar 相关抗体:
体内研究
(In Vivo)

PET scans with the Pgp substrate (R)-[11C]NSC 657799 in FVB wild-type mice pretreated i.v. with Encequidar (HM30181) (10 or 21 mg/kg) failes to show significant increases in (R)-[11C]NSC 657799 brain uptake compared with vehicle treated animals[1].
Encequidar (HM30181) inhibits P-gp mainly in the intestinal endothelium, which can be beneficial because pan-inhibition of P-gp, particularly in the brain, could lead to detrimental adverse events. Encequidar (HM30181) increases the oral bioavailability of co-administered NSC 125973 by more than 12 times in rats[2].

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

688.73

Formula

C38H36N6O7
CAS 号
性状

固体

颜色

Light yellow to yellow

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 : 2.4 mg/mL (3.48 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4519 mL 7.2597 mL 14.5195 mL
5 mM --- --- ---
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
参考文献
Animal Administration
[1]

Mice[1]
Encequidar (HM30181) mesylate is dissolved in 5% aqueous glucose solution, containing 20 μL 0.01 M aq. HCl and injected at a volume of 4 mL/kg. Female FVB wild-type mice, aged 8-12 weeks weighing 24±4 g undergo (R)-[11C]NSC 657799 PET scans without and with i.v. pretreatment with cold Encequidar (HM30181). Animals are assigned to 5 groups (n=4 per group). One group is pretreated with HM30181 vehicle solution (5% aq. glucose solution containing 20 μL 0.01 M aq. HCl) at 60 min before start of the PET scan. The other groups are pretreated with either 10 mg/kg Encequidar (HM30181) at 10, 60 or 120 min before PET or with 21 mg/kg HM30181 at 10 min before PET[1].

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

Encequidar 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 1.4519 mL 7.2597 mL 14.5195 mL 36.2987 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:

Encequidar849675-66-7HM30181 HM30181AHM 30181HM-30181P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

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