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HM30181 mesylate (Encequidar mesylate)

产品编号: DC12074 Featured
HM30181 mesylate (Encequidar mesylate)
结构式
849675-87-2
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中国地区超过5000个高品质化合物库存
应用领域
HM30181 mesylate is a competitive and potent P-glycoprotein inhibitor.
化学性质生物活性化合物的使用COA & MSDS相关产品产品说明书
Cas No.: 849675-87-2
名称:
别名:
SMILES: O=C(C1=CC(C2=CC=CC=C2O1)=O)NC3=CC(OC)=C(OC)C=C3C4=NN(C5=CC=C(CCN6CC7=C(C=C(OC)C(OC)=C7)CC6)C=C5)N=N4.CS(=O)(O)=O
分子式: C39H40N6O10S
分子量: 784.83
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: In Vitro Compared with control (0 nM HM30181A), paclitaxel potently inhibits the survival of K1735 cells by about 65% at 100 nM and 72% at 1000 nM in a dose-dependent manner. HM30181A does not make any significant changes in the survival of K1735 cells. In contrast, bEnd.3 cells do not show any decreases in survival by the paclitaxel treatment without HM30181A. However, treatment of 0.1 or 1 nM HM30181A lead to 20 and 42% inhibition of survival at the 100 nM and 1000 nM paclitaxel treatment, respectively. In Vivo The plasma concentrations of HM30181M are higher for the simultaneous administration with the microcapsule than with the powder; providing significant differences from 1 to 2 h (p < 0.05). The microcapsule has about a 1.7-fold faster Tmax and a 1.6-fold higher AUC value compared with the powder (2.5±0.6 vs. 4.3±0.9 h; 107.7±20.1 vs. 64.3±18.0 h ng/mL). The faster and overall improved absorption of HM30181M in microcapsule form might be due to the remarkable enhancement of the aqueous solubility and dissolution resulting from its crystalline conversion to the amorphous form and particle size reduction.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
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MSDS_3200_DC12074_849675-87-2
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