Elacridar hydrochloride (GF120918A) 是一种具有口服活性的的P-glycoprotein (P-gp)和乳腺癌抗性蛋白 (BCRP)抑制剂。Elacridar hydrochloride 可用于检测外排转运体对药物脑内分布的影响，并可用于癌症的研究。
| 生物活性 | Elacridar hydrochloride (GF120918A) is an orally activeP-glycoprotein(P-gp)andbreastcancerresistance protein (BCRP)inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on drug distribution to brain and it can be used for the research ofcancer[1][2]. |
体外研究
(In Vitro) | Elacridar hydrochloride (0.001-1 μM; 2 h) inhibits cell viability of 786-O cells[2].Elacridar hydrochloride (5 μM; 24 h) affects P-glycoprotein and ABCG2 protein expression levels in MCF-7 and 786-O cell lines[2].Elacridar hydrochloride (5 μM; 24 h) affects99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells[2].
Cell Viability Assay[2] | Cell Line: | 786-O cells | | Concentration: | 2.5 and 5 μM | | Incubation Time: | 2 hours | | Result: | Dose-dependently inhibited cell viability of 786-O cells and showed better inhibitory effect with sunitnib adding. |
Western Blot Analysis[2] | Cell Line: | MCF-7, Caki-1, and 786-O cell lines | | Concentration: | 5 μM | | Incubation Time: | 24 hours | | Result: | Dreased P-glycoprotein protein expression level in 786-O cells and increased ABCG2 protein expression level in Caki-1 cells. |
Cell Viability Assay[2] | Cell Line: | MCF-7 and 786-O cell lines | | Concentration: | 5 μM | | Incubation Time: | 24 hours | | Result: | Dose-dependently increased99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells. |
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体内研究
(In Vivo) | Elacridar hydrochloride (100 mg/kg; i.p. once) shows different distribution in brain and plasma[1]. 1.19Plasma Pharmacokinetic Parameters of Elacridar hydrochloride in mice[1]. | Mice
PO 100 mg/kg | Mice
IP 100 mg/kg | Mice
IV 2.5 mg/kg | | CL/F (ml/min) | 2.05 | 33.2 | 0.46 | | Vd/F (liter) | 3.5 | 12.3 | 0.17 | | t1/2(h) | 20 | 4.3 | 4.4 | | AUC0-inf(μg·min/ml) | 1460 | 90.3 | 161.4 | | F | 0.22 | 0.013 | 1 |
| Animal Model: | FVB wild-type mice[1] | | Dosage: | 100 mg/kg | | Administration: | Intraperitoneal injection; 100 mg/kg once | | Result: | Showd a higher concertration in brain than plasma except at 4 h after administration. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 62.5 mg/mL(104.15 mM;Need ultrasonic) H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble) 配制储备液 | 1 mM | 1.6664 mL | 8.3319 mL | 16.6639 mL | | 5 mM | 0.3333 mL | 1.6664 mL | 3.3328 mL | | 10 mM | 0.1666 mL | 0.8332 mL | 1.6664 mL |
*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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 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 40%PEG300 5%Tween-80 45% saline Solubility: 2.08 mg/mL (3.47 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (3.47 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 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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