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Tariquidar methanesulfonate, hydrate

产品编号 T13087 CAS 625375-83-9

别名: XR9576 methanesulfonate, hydrate

Tariquidar methanesulfonate, hydrate is a potent and specific P-glycoprotein (P-gp) inhibitor(Kd of 5.1 nM).

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Tariquidar methanesulfonate, hydrate Chemical Structure

Tariquidar methanesulfonate, hydrate, CAS 625375-83-9

规格	价格/CNY		货期	数量
500 mg	￥ 10,900		待询

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Tariquidar methanesulfonate, hydrate 的其他形式现货产品:

Tariquidar

其他形式的 Tariquidar methanesulfonate, hydrate:

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Tariquidar methanesulfonate, hydrate is a potent and specific P-glycoprotein (P-gp) inhibitor(Kd of 5.1 nM).
靶点活性	P-gp:(kd)5.1 nM
体外活性	Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) is a potent P-gp mediated [3H]-Vinblastine modulator and [3H]-Paclitaxel transport as it increases the steady-state accumulation of these cytotoxics in CHrB30 cells to levels observed in non-P-gp-expressing AuxB1 cells with EC50 of 487±50 nM. [3H]-Tariquidar binds to CHrB30 membranes with the highest affinity with Kd of 5.1±0.9 nM, n=7 and a binding capacity (Bmax) of 275±15 pmol/mg membrane protein. In contrast to the parental cell line, the accumulation of [3H]-Vinblastine is increased in a dose-dependent fashion by the modulators XR9576 with EC50 of 487±50 nM. The MDR modulator Tariquidar is able to inhibit 60-70% of the vanadate-sensitive ATPase activity(IC50 of 43±9 nM)[1]. Tariquidar potentiates the cytotoxicity of several drugs including Doxorubicin, Paclitaxel, Etoposide, and Vincristine; complete reversal of resistance is achieved in the presence of 25-80 nM Tariquidar. Tariquidar is a potent inhibitor of photoaffinity labeling of P-gp by [3H]Azidopine implying a direct interaction with the protein[2].
体内活性	In mice with intrinsically resistant MC26 colon tumors, co-administration of hydrated Tariquidar mesylate (XR9576 mesylate, hydrate) can enhance the antitumor activity of doxorubicin without significantly increasing toxicity; maximum potentiation is observed at 2.5-4.0 mg/kg dosed either i.v. or p.o. In addition, coadministration of Tariquidar (6-12 mg/kg p.o.) fully restores the antitumor activity of Paclitaxel, Etoposide, and Vincristine against two highly resistant MDR human tumor xenografts (2780AD, H69/LX4) in nude mice. Tariquidar is found to also significantly potentiate the antitumor activity of doxorubicin against s.c. MC26 tumors in vivo[2].

别名	XR9576 methanesulfonate, hydrate
分子量	892.99
分子式	C40H52N4O15S2
CAS No.	625375-83-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 296 mg/mL (331.47 mM)

H2O: 5 mg/mL (5.60 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / H2O	1 mM	1.1198 mL	5.5992 mL	11.1983 mL	27.9958 mL
DMSO / H2O	5 mM	0.224 mL	1.1198 mL	2.2397 mL	5.5992 mL
DMSO	10 mM	0.112 mL	0.5599 mL	1.1198 mL	2.7996 mL
	20 mM	0.056 mL	0.28 mL	0.5599 mL	1.3998 mL
	50 mM	0.0224 mL	0.112 mL	0.224 mL	0.5599 mL
	100 mM	0.0112 mL	0.056 mL	0.112 mL	0.28 mL

计算器

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参考文献

1. Martin C, et al. The molecular interaction of the high affinity reversal agent XR9576 with P-glycoprotein. Br J Pharmacol, 1999, 128(2), 403-411. 2. Mistry P, et al. In vitro and in vivo reversal of P-glycoprotein-mediated multidrug resistance by a novel potent modulator, XR9576. Cancer Res, 2001, 61(2), 749-758. 3. Vraka C, et al. A new method measuring the interaction of radiotracers with the human P-glycoprotein (P-gp) transporter. Nucl Med Biol. 2018 Feb 14;60:29-36.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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