Tariquidar (methanesulfonate, hydrate)

中文名	Tariquidar (methanesulfonate, hydrate)
英文名	Tariquidar (methanesulfonate, hydrate)
别名	P-糖蛋白抑制剂化合物 T13087 他立喹达二甲磺酸盐六水合物 TARIQUIDAR 二甲磺酸盐六水合物
英文别名	XR9576 XR-9576 XR 9576 Tariquidar methanesulfonate XR9576 methanesulfonate, hydrate TARIQUIDAR METHANESULFONATE HYDRATE Tariquidar (methanesulfonate, hydrate) Tariquidar (Methanesulfonate, hydrate) Tariquidar dimethanesulfonate hexahydrate Tariquidar methanesulfonate hydrate (XR9576) N-[2-({4-[2-(6,7-Dimethoxy-3,4-dihydro-2(1H)-isoquinolinyl)ethyl]phenyl}carbamoyl)-4,5-dimethoxyphenyl]-3-quinolinecarboxamide
CAS	625375-83-9
化学式	C40H52N4O15S2
分子量	892.98868
溶解度	DMSO: ≥ 296 mg/mL; H₂O: < 8.9 mg/mL
存储条件	-20℃
体外研究	Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) is a potent modulator of P-gp mediated [ 3 H]-Vinblastine and [ 3 H]-Paclitaxel transport as it increases the steady-state accumulation of these cytotoxics in CH r B30 cells to levels observed in non-P-gp-expressing AuxB1 cells (EC 50 =487±50 nM). [ 3 H]-Tariquidar binds to CH r B30 membranes with the highest affinity (K d =5.1±0.9 nM, n=7) and a binding capacity (B max ) of 275±15 pmol/mg membrane protein. In contrast to the parental cell line, the accumulation of [ 3 H]-Vinblastine is increased in a dose-dependent fashion by the modulators XR9576 (EC 50 =487±50 nM). The MDR modulator Tariquidar is able to inhibit 60-70% of the vanadate-sensitive ATPase activity, with potent IC 50 value of 43±9 nM. Tariquidar (XR9576) 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 [ 3 H]Azidopine implying a direct interaction with the protein.
体内研究	In mice bearing the intrinsically resistant MC26 colon tumors, coadministration of Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) potentiates the antitumor activity of Doxorubicin without a significant increase in 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.

Tariquidar (methanesulfonate, hydrate) - 配置溶液浓度参考

	1mg	5mg	10mg
1 mM	1.12 ml	5.599 ml	11.198 ml
5 mM	0.224 ml	1.12 ml	2.24 ml
10 mM	0.112 ml	0.56 ml	1.12 ml
5 mM	0.022 ml	0.112 ml	0.224 ml

最后更新：2024-01-02 23:10:35

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产品名: 他立喹达二甲磺酸盐六水合物去供应商网站查看询盘
CAS: 625375-83-9
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产品描述: 中文名：他立喹达二甲磺酸盐六水合物英文名:Tariquidar methanesulfonate, hydrate CAS:625375-83-9 规格:98 更多

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产品名: Tariquidar methanesulfonate, hydrate 去供应商网站查看询盘
CAS: 625375-83-9
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价格: 10mg-904,50mg-2785
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产品名: Tariquidar (methanesulfonate, hydrate) 去供应商网站查看询盘
CAS: 625375-83-9
产地: 上海
规格: 98%
价格: 10mg 950,50mg 2930,100mg 4600
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