Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor.

P-glycoprotein^[1][2].

Treatment of 0.1 or 1 nM Encequidar (HM30181) lead to 20 and 42% inhibition of survival at the 100 nM and 1000 nM NSC 125973 treatment, respectively^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

The plasma concentrations of Encequidar (HM30181) are higher for the simultaneous administration with the microcapsule than with the powder; providing significant differences from 1 to 2 h. The microcapsule has about a 1.7-fold faster T_max and a 1.6-fold higher AUC value compared with the powder (2.5±0.6 vs. 4.3±0.9 h; 107.7±20.1 vs. 64.3±18.0 h ng/mL). The faster and overall improved absorption of Encequidar (HM30181) in microcapsule form might be due to the remarkable enhancement of the aqueous solubility and dissolution resulting from its crystalline conversion to the amorphous form and particle size reduction^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

784.83

C₃₉H₄₀N₆O₁₀S

849675-87-2

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

DMSO : 25 mg/mL (31.85 mM; Need ultrasonic)

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: 2.5 mg/mL (3.19 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (3.19 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

• [1]. Kim JC, et al. Effect of HM30181 mesylate salt-loaded microcapsules on the oral absorption of NSC 125973 as a novel P-glycoprotein inhibitor. Int J Pharm. 2016 Jun 15;506(1-2):93-101.

  [2]. Joo KM, et al. Response of brain specific microenvironment to P-glycoprotein inhibitor: an important factor determining therapeutic effect of P-glycoprotein inhibitor on brain metastatic tumors. Int J Oncol. 2008 Oct;33(4):705-12.

Rats^[1]
The cannulised rats are divided into four groups, each comprises of 6 rats. Encequidar (HM30181) powder or Encequidar (HM30181)- loaded microcapsules are enclosed in hard capsules. One group of rats is dosed orally with NSC 125973 solution only, at a drug dose of 20 mg/kg. The rats in the other two groups are administered NSC 125973 solution at a drug dose of 20 mg/kg simultaneously with either capsules containing Encequidar (HM30181) powder or microcapsules (equivalent to 20 mg/kg Encequidar (HM30181))^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Kim JC, et al. Effect of HM30181 mesylate salt-loaded microcapsules on the oral absorption of NSC 125973 as a novel P-glycoprotein inhibitor. Int J Pharm. 2016 Jun 15;506(1-2):93-101.

  [2]. Joo KM, et al. Response of brain specific microenvironment to P-glycoprotein inhibitor: an important factor determining therapeutic effect of P-glycoprotein inhibitor on brain metastatic tumors. Int J Oncol. 2008 Oct;33(4):705-12.