Elacridar 是一种具有口服活性的的P-glycoprotein (Pgp)和乳腺癌抗性蛋白 (BCRP)抑制剂。Elacridar 可用于检测外排转运体对药物脑内分布的影响以及癌症的研究。
| 生物活性 | Elacridar is an orally activeP-glycoprotein(Pgp)andbreastcancerresistance protein (BCRP)inhibitor. Elacridar can be used to examine the influence of efflux transporters on drug distribution to brain and the research ofcancer[1][2]. |
| IC50& Target | P-glycoprotein (Pgp), BCRP[1] |
体外研究
(In Vitro) | Elacridar (0.001-1 μM; 2 h) inhibits cell viability of 786-O cells[2].Elacridar (5 μM; 24 h) affects P-glycoprotein and ABCG2 protein expression levels in MCF-7 and 786-O cell lines[2].Elacridar (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 (100 mg/kg; i.p. once) shows different distribution in brain and plasma[1]. 1.19
Plasma Pharmacokinetic Parameters of Elacridar 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(μgomin/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 the dose. |
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| 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 | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 5 mg/mL(8.87 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.7742 mL | 8.8709 mL | 17.7418 mL | | 5 mM | 0.3548 mL | 1.7742 mL | 3.5484 mL | | 10 mM | --- | --- | --- |
*请根据半岛bd体育手机客户端
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半岛bd体育手机客户端
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-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 90% (20%SBE-β-CDin saline) Solubility: 1.67 mg/mL (2.96 mM); Suspended solution; Need ultrasonic
此方案可获得 1.67 mg/mL (2.96 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 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 0.5 mg/mL (0.89 mM); Clear solution
此方案可获得 ≥ 0.5 mg/mL (0.89 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 5.0 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。 3. 请依序添加每种溶剂： 5% DMSO 40%PEG300 5%Tween-80 50% saline Solubility: ≥ 0.25 mg/mL (0.44 mM); Clear solution 4. 请依序添加每种溶剂： 5% DMSO 95% (20%SBE-β-CDin saline) Solubility: 0.25 mg/mL (0.44 mM); Suspended solution; Need ultrasonic 5. 请依序添加每种溶剂： 1% DMSO 99% saline Solubility: 0.05 mg/mL (0.09 mM); Suspended solution; Need ultrasonic *以上所有助溶剂都可在本网站选购。
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