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Tariquidar/他立喹达 {[allProObj[0].p_purity_real_show]}

货号：A251517 同义名： XR9576

Tariquidar 是一种有效且选择性非竞争性 P-糖蛋白抑制剂，Kd 为 5.1 nM，可逆转 MDR 细胞系中的药物耐药性。

Tariquidar/他立喹达 化学结构 CAS号：206873-63-4
Tariquidar/他立喹达 化学结构
CAS号：206873-63-4
Tariquidar/他立喹达 3D分子结构
CAS号：206873-63-4
Tariquidar/他立喹达 化学结构 CAS号：206873-63-4
Tariquidar/他立喹达 3D分子结构 CAS号：206873-63-4
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Tariquidar/他立喹达 纯度/质量文件 产品仅供科研

货号：A251517 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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产品名称 P-gp ↓ 其他靶点 纯度
Elacridar ✔ BCRP 99%+
Zosuquidar 3HCl ++

P-gp, Ki: 60 nM

 		99%+
SC144 ✔ 99%+
Tariquidar +++

P-gp, Kd: 5.1 nM

 		98%
Schizandrin B ✔ 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Tariquidar/他立喹达 生物活性

靶点

  • P-gp

    P-gp, Kd:5.1 nM
描述 The multidrug resistance is an obstacle in the chemotherapy treatment (such as doxorubicin, vincristine, paclitaxel, TKIs) for many solid and haematological tumours. Many factors can cause the multidrug resistance. Among them, the overexpression of P-gp (ABCB1), of which vinblastine and paclitaxel is the substrate, on the surface of resistant cells is considered as a key factor mediating multidrug resistance. Thus, the increased bioavailable and brain accumulation of anticancer drugs can be achieved partially through inhibition of P-gp. Tariquidar is a potent P-gp transport modulator with IC50 value of 0.4μM, displaying specific high-affinity binding to P-gp with Kd of 5.1nM. The cellular study showed that the accumulation of vinblastine and paclitaxel can be increased in a dose-dependent manner by tariquidar with EC50 value of 487nM and 25.4nM, respectively, in CHrB30 cells, not mediated through competition for transport[1]. Co-administration of paclitaxel with tariquidar (p.o., 50mg/kg) led to a comparable increase and a long lasting 5-fold increase in the concentration of paclitaxel accumulation in the cytostatic in the brain of nude mice[2].
作用机制 Tariquidar can bind at a site which is distinct from the site of interaction of transport substrates and alter P-gp-mediated transport by affecting its rate of ATP hydrolysis.[1]

Tariquidar/他立喹达 细胞实验

Cell Line
Concentration Treated Time Description References
eIMS cells 100 nM 72 h Tariquidar restored BV sensitivity in BV-treated eIMS cells, significantly reducing the GI50 value. Br J Cancer. 2020 Sep;123(7):1101-1113.
S. mansoni adult worms 10 μM Enhance uptake and retention of TGR inhibitors, improving adult worm killing efficacy Nat Commun. 2023 Jun 22;14(1):3737.
NCI-ADR-RES cells 1 μM 72 h Restored the antiproliferative effect of LY3023414 in ABCB1-overexpressing NCI-ADR-RES cells Biochem Pharmacol. 2020 Oct;180:114137.
MDR19-HEK293 cells 1 μM 72 h Restored the antiproliferative effect of LY3023414 in ABCB1-overexpressing MDR19-HEK293 cells Biochem Pharmacol. 2020 Oct;180:114137.
Plasmodium yoelii NSRNT/ubp1::mCherry 100 nM 10 min Inhibition of MDR1 transport, increasing Fluo-4 accumulation in the parasite cytosol Nat Commun. 2024 Feb 27;15(1):1774.
Plasmodium yoelii NSSIP/ubp1::mCherry 100 nM 10 min Inhibition of MDR1 transport, decreasing Fluo-4 accumulation in the parasite cytosol Nat Commun. 2024 Feb 27;15(1):1774.

Tariquidar/他立喹达 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice EIMS xenograft models Oral 12 mg/kg Twice weekly for 6 weeks Combination treatment with tariquidar and BV prolonged the survival of mice but only slightly slowed tumour growth. Br J Cancer. 2020 Sep;123(7):1101-1113.
Mice Plasmodium yoelii infected mouse model Intraperitoneal injection 12 mg/kg Once daily for four days Tariquidar in combination with antimalarial drugs significantly reduced parasitemia, reversing UBP1NT-mediated multidrug resistance Nat Commun. 2024 Feb 27;15(1):1774.

Tariquidar/他立喹达 动物研究

Dose Rat[3] (i.v.): 1 mg/kg - 15 mg/kg; Mice[4] (i.p.): 6.5 mg/kg - 13 mg/kg; Mice[5] (p.o.): 6 mg/kg - 12 mg/kg
Administration i.v., i.p., p.o.
Pharmacokinetics
Animal Rats[6]
Dose 15 mg/kg
Administration i.v.
p.o.
i.p.
F 71.6% (p.o.)
91.4% (i.p.)
AUC0→24h 25.2 μg·h/ml (i.v.)
18.1 μg·h/ml (p.o.)
23.8 μg·h/ml (i.p.)
Tmax 0.5 μg/ml (i.v.)
4.0 μg/ml (p.o.)
2.0 μg/ml (i.p.)
Cmax 1.9 μg/ml (i.v.)
1.2 μg/ml (p.o.)
1.5 μg/ml (i.p.)

Tariquidar/他立喹达 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01663545 - Completed - United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 收起 <<
NCT01547754 - Terminated - United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 收起 <<
NCT01386476 - Completed - United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 收起 <<

Tariquidar/他立喹达 参考文献

[1]Hubensack M, M¨¹ller C, et al. Effect of the ABCB1 modulators elacridar and tariquidar on the distribution of paclitaxel in nude mice. J Cancer Res Clin Oncol. 2008 May;134(5):597-607. Epub 2007 Oct 12.

[2]Martin C, Berridge G, et al. The molecular interaction of the high affinity reversal agent XR9576 with P-glycoprotein. Br J Pharmacol. 1999 Sep;128(2):403-11

[3]Bankstahl JP, Kuntner C, et al. Tariquidar-induced P-glycoprotein inhibition at the rat blood-brain barrier studied with (R)-11C-verapamil and PET. J Nucl Med. 2008 Aug;49(8):1328-35.

[4]Foran E, Kwon DY, et al. CNS uptake of bortezomib is enhanced by P-glycoprotein inhibition: implications for spinal muscular atrophy. Neurobiol Dis. 2016 Apr;88:118-24.

[5]Mistry P, Stewart AJ, et al. In vitro and in vivo reversal of P-glycoprotein-mediated multidrug resistance by a novel potent modulator, XR9576. Cancer Res. 2001 Jan 15;61(2):749-58.

[6]Matzneller P, Kussmann M, et al. Pharmacokinetics of the P-gp Inhibitor Tariquidar in Rats After Intravenous, Oral, and Intraperitoneal Administration. Eur J Drug Metab Pharmacokinet. 2018 Oct;43(5):599-606.

Tariquidar/他立喹达 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.55mL

0.31mL

0.15mL

7.73mL

1.55mL

0.77mL

15.46mL

3.09mL

1.55mL

Tariquidar/他立喹达 技术信息

CAS号206873-63-4
分子式C38H38N4O6
分子量 646.73
SMILES Code O=C(C1=CC2=CC=CC=C2N=C1)NC3=CC(OC)=C(OC)C=C3C(NC4=CC=C(CCN5CC6=C(C=C(OC)C(OC)=C6)CC5)C=C4)=O
MDL No. MFCD09837824
别名 XR9576
运输蓝冰
InChI Key LGGHDPFKSSRQNS-UHFFFAOYSA-N
Pubchem ID 148201
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C
溶解方案

DMSO: 15 mg/mL(23.19 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一

Tags: Tariquidar | 206873-63-4 | XR9576 | XR 9576 | XR-9576 | P-gp Inhibitor | Membrane Transporter/Ion Channel | P-glycoprotein | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Tariquidar/他立喹达 纯度/质量文件 | Tariquidar/他立喹达 亚型比较 | Tariquidar/他立喹达 生物活性 | Tariquidar/他立喹达 动物研究 | Tariquidar/他立喹达 临床数据 | Tariquidar/他立喹达 参考文献 | Tariquidar/他立喹达 实验方案 | Tariquidar/他立喹达 技术信息

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