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Elacridar hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Elacridar hydrochloride图片
CAS NO:143851-98-3
包装与价格:
包装价格(元)
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
GF120918A
产品介绍
Elacridar hydrochloride (GF120918A) 是一种具有口服活性的的P-glycoprotein (P-gp)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.
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)2.0533.20.46
Vd/F (liter)3.512.30.17
t1/2(h)204.34.4
AUC0-inf(μg·min/ml)146090.3161.4
F0.220.0131

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.
分子量

600.10

性状

Solid

Formula

C34H34ClN3O5

CAS 号

143851-98-3

中文名称

依克立达盐酸盐

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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.6664 mL8.3319 mL16.6639 mL
5 mM0.3333 mL1.6664 mL3.3328 mL
10 mM0.1666 mL0.8332 mL1.6664 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
*以上所有助溶剂都可在本网站选购。