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LY335979 trihydrochloride

目录号 M1845 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


Zosuquidar (LY335979) 3HCl是一种有效的P-glycoprotein(P-糖蛋白)介导的多药耐抗性的调节剂,Ki为60 nM。

LY335979 trihydrochloride结构式

别名:Zosuquidar trihydrochloride

规格 价格 库存状态
Free Sample (0.5-1 mg)  ¥ 0 中国库存现货
2mg ¥ 520 中国库存现货
5mg ¥ 936 中国库存现货
10mg ¥ 1430 中国库存现货
25mg ¥ 2990 中国库存现货
其他规格数量报价?

质量标准及产品资料
生物活性

Zosuquidar (LY335979) 3HCl是一种有效的P-glycoprotein(P-糖蛋白)介导的多药耐抗性的调节剂,Ki为60 nM。LY335979 竞争性抑制[3H]vinblastine与P-gp的平衡结合,Ki为 60 nM,通过阻断CEM/VLB100质膜中P-gp的[3H]azidopine的光亲和标记。LY335979 浓度为0.1 μM时,单独给药对药物敏感的MDR细胞系,具有细胞毒性,IC50为6 μM-16 μM,且浓度为 0.5 μM时,完全扭转对 MDR 细胞P388/ADR, MCF7/ADR, 2780AD, 或 UCLA-P3.003VLB溶瘤细胞抗性(Vinblastine, Doxorubicin, 或 Etoposide)。LY335979作用于表达P-gp的白血病细胞系,包括K562/HHT40, K562/HHT90, K562/DOX 和 HL60/DNR,显著恢复药物敏感性,且作用于携带活性P-gp的原发性AML细胞,增强蒽环类药物(Daunorubicin, Idarubicin, Mitoxantrone)和gemtuzumab ozogamicin 的毒性。

产品使用成果展示
数据来源 Drug Metab Dispos (2017). Figure 1. LY335979
方法 Construction of MDCKII Monolayers Expressing BCRP or BCRP1
细胞系/动物模型 MDCKII cells
浓度 1 µM
处理时间 -
实验结果 Inclusion of 1 µM of P-gp–specific inhibitor LY335979 in transport medium completely inhibited endogenous P-gp activity, with no effect on BCRP1 activity in MDCKII cells
实验参考
体外实验*
细胞系 MCF-7 and MCF-7/ADR cells
方法 Cytotoxicity Assays.
Cell viability was determined using a modified 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide dye reduction method. Cells were harvested during logarithmic growth phase, and seeded in 96-well plates (Costar) at 7.5X104 cells/well. The cells were then cultured for 72 h in the presence of oncolytics with or without modulators. MCF-7 and MCF-7/ADR cells were incubated 24 h before the addition of the drug with and without the modulator. Modulators were prepared as 2 mM DMSO stocks and added to wells to give final concentrations ranging from 0.05 to 5 uM. After 72 h, 20 ul of freshly prepared 3-(4,5-dimethylthiazol-2- yl)-2,5-diphenyltetrazolium bromide (5 mg/mL in Dulbecco's PBS) was added to each well and incubated for 4 h in a 37°C incubator containing 5% CO2. Cells were pelleted in a Sorvall RT6000B centrifuge, 70 p.1of medium was carefully removed from each well, and 100ul of 2-propanol/0.04 N HC1 was added. Cells were resuspended 5-10 times with a Multipipettor or until no particulate matter was visible. Plates were immediately read on a Titertek Multiskan MCC/340 microplate reader Flow Laboratories (McLean, VA) with a test wavelength of 570 nm and a reference wavelength of 630 nm.Controls were measured in quadruplicate and modulators were measured in duplicate. Cytotoxicity analyses were also performed using the CeliTiter 96 AQueous assay kit (Promega Corp., Madison, WI) according to the manufacturer's instructions.
浓度 0.05~5µM
处理时间 72h

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

体内实验*
动物模型 P388/ADR tumors bearing mice
配制 stock solution was 2.5 to 5 mg/nil in 5% manrntol
剂量 20 mg/kg once daily for 5 days
给药处理 i.v. injection

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

化学性质
分子量 637.00
分子式 C32H31F2N3O2.3HCl
CAS号 167465-36-3
溶解性(25°C) DMSO ≥35 mg/mL
储存条件 粉末型式       -20°C   3年;4°C   2年
溶于溶剂       -80°C   6个月;-20°C   1个月
运输方式 冰袋运输,根据产品的不同,可能会有相应调整。
储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.5699 mL 7.8493 mL 15.6986 mL
5 mM 0.314 mL 1.5699 mL 3.1397 mL
10 mM 0.157 mL 0.7849 mL 1.5699 mL
不同实验动物依据体表面积的等效剂量转换表(参考来源于公开文献
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Mease et al. J Pharm Sci. Differential selectivity of efflux transporter inhibitors in Caco-2 and MDCK-MDR1 monolayers: a strategy to assess the interaction of a new chemical entity with P-gp, BCRP, and MRP2.

[2] Abu Ajaj et al. Breast Cancer Res Treat. Zosuquidar and an albumin-binding prodrug of zosuquidar reverse multidrug resistance in breast cancer cells of doxorubicin and an albumin-binding prodrug of doxorubicin.

[3] Fuchs et al. Eur J Pharm Sci. Excretion of the dipeptidyl peptidase-4 inhibitor linagliptin in rats is primarily by biliary excretion and P-gp-mediated efflux.

[4] Cripe et al. Blood. Zosuquidar, a novel modulator of P-glycoprotein, does not improve the outcome of older patients with newly diagnosed acute myeloid leukemia: a randomized, placebo-controlled trial of the Eastern Cooperative Oncology Group 3999.

[5] Dantzig AH, et al. Cancer Res. Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979.

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