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Encequidar {[allProObj[0].p_purity_real_show]}

货号:A658719 同义名: HM30181; HM30181A

Encequidar是一种选择性的P-glycoprotein(P-gp)抑制剂,用于增强药物在肿瘤细胞中的积累。该化合物具有强效的选择性作用,并可作为化疗药物的辅助治疗。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Encequidar 化学结构 CAS号:849675-66-7
Encequidar 化学结构
CAS号:849675-66-7
Encequidar 3D分子结构
CAS号:849675-66-7
Encequidar 化学结构 CAS号:849675-66-7
Encequidar 3D分子结构 CAS号:849675-66-7
规格 价格 会员价 库存 数量
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Encequidar 纯度/质量文件 产品仅供科研

货号:A658719 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 P-gp 其他靶点 纯度
Elacridar BCRP 99%+
Zosuquidar 3HCl ++

P-gp, Ki: 60 nM

99%+
SC144 99%+
Tariquidar +++

P-gp, Kd: 5.1 nM

98%
Schizandrin B 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Encequidar 生物活性

描述 Encequidar demonstrates comparable potency to the reference Pgp inhibitor tariquidar in blocking rhodamine 123 efflux from CCRF-CEM T cells (IC50, tariquidar: 8.2±2.0 nM, Encequidar: 13.1±2.3 nM) [1]. Encequidar (HM30181) exhibits high selectivity for mP-gp, with a potency 20-50 times greater than that of tariquidar, another third-generation P-gp inhibitor[2].
体内研究

PET scans using the Pgp substrate (R)-[11C]NSC 657799 in FVB wild-type mice pretreated intravenously with Encequidar (HM30181) (at doses of 10 or 21 mg/kg) did not demonstrate significant increases in (R)-[11C]NSC 657799 brain uptake compared to vehicle-treated animals[1].

Encequidar primarily inhibits P-gp in the intestinal endothelium, offering potential benefits by avoiding widespread P-gp inhibition, especially in the brain, which could trigger adverse effects. Encequidar (HM30181) enhances the oral bioavailability of co-administered NSC 125973 by over 12-fold in rats[2].

体外研究

Encequidar demonstrates comparable potency to the reference Pgp inhibitor tariquidar in blocking rhodamine 123 efflux from CCRF-CEM T cells (IC50, tariquidar: 8.2±2.0 nM, Encequidar: 13.1±2.3 nM) [1].

Encequidar (HM30181) exhibits high selectivity for mP-gp, with a potency 20-50 times greater than that of tariquidar, another third-generation P-gp inhibitor[2].

Encequidar 参考文献

[1]Bauer F, et al. Interaction of HM30181 with P-glycoprotein at the murine blood-brain barrier assessed with positron emission tomography. Eur J Pharmacol. 2012 Dec 5;696(1-3):18-27.

[2]Kim TE, et al. Effects of HM30181, a P-glycoprotein inhibitor, on the pharmacokinetics and pharmacodynamics of loperamide in healthy volunteers. Br J Clin Pharmacol. 2014 Sep;78(3):556-64.

Encequidar 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.45mL

0.29mL

0.15mL

7.26mL

1.45mL

0.73mL

14.52mL

2.90mL

1.45mL

Encequidar 技术信息

CAS号849675-66-7
分子式C38H36N6O7
分子量 688.73
SMILES Code O=C(C1=CC(C2=CC=CC=C2O1)=O)NC3=CC(OC)=C(OC)C=C3C4=NN(C5=CC=C(CCN6CC7=C(C=C(OC)C(OC)=C7)CC6)C=C5)N=N4
MDL No. MFCD25976625
别名 HM30181; HM30181A
运输蓝冰
InChI Key AHJUHHDDCJQACA-UHFFFAOYSA-N
Pubchem ID 11399764
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, store in freezer, under -20°C

溶解方案

DMSO: 2 mg/mL(2.9 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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