Elacridar (Synonyms:GF120918; GW0918; GG918; GW120918)
目录号 : KM16628 CAS No. : 143664-11-3 纯度 : 98%

Elacridar (GF120918) 是一种有效的 P-糖蛋白 (P-glycoprotein) 和 BCRP 的抑制剂。

规格 价格 是否有货 数量
10mg
In-stock
50mg
In-stock
100mg
In-stock
200mg
In-stock
500mg
In-stock
1g 询价 In-stock
5g 询价 In-stock

Other Forms of Rapamycin:

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生物活性

Elacridar (GF120918) is a potent P-glycoprotein (Pgp) and BCRP inhibitor.

体外研究

Elacridar inhibits P-glycoprotein (P-gp) labeling by [H]azidopine with a IC50 of 0.16 μM. In Caki-1 and ACHN cells, elacridar (2.5 μM) significantly ihibits the cell growth. The P-glycoprotein activity is found to be inhibited by elacridar. The combination of elacridar and SU 11248 lead to a significant reduction in ABC Sub-family B Member 2 (ABCG2) expression in 786-O cells.

体内研究

Oral co-administration of elacridar (100 mg/kg, p.o.) and PF-02341066 increases the plasma and brain concentrations and brain-to-plasma ratios of PF-02341066 in wild-type mice, equaling the levels in Abcb1a/1b; Abcg2 mice. In friend leukemia virus stain B mice, the brain-to-plasm partition coefficient (Kp, brain) of elacridar is 0.82, 0.43, and 4.31 after intravenous (2.5 mg/kg), intraperitoneal (100 mg/kg), and oral (100 mg/kg) treatment, respectively. In Mrp4(-/-) mice, elacridar fully inhibits P-gp mediated transport of SKF 104864A, without siginificant effects on Bcrp1-mediated transport.

分子式
C34H33N3O5
分子量
563.64
CAS号
143664-11-3
中文名称
依克立达
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
溶解性数据
In Vitro: 

DMSO : 5 mg/mL (8.87 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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。-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。

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-CD in 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 μL 20% 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-CD in 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

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