MK-571 sodium

CAS号

115103-85-0

分子式

C26H27ClN2O3S2·Na

主要靶点

LTR|Leukotriene Receptor

仅限科研使用

Cat No : CM05005

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Synonyms

pulmonary hypertension|RBL-2H3 cells|L 660711|LAD2|L-660711 (sodium salt)|L-660711 sodium|L-660711 sodium salt|L660711|MK 571 sodium|MK 571|MK-571 sodium salt|MK571|MK-571|MK571 sodium|MK-571 sodium|MRP1|MRP4|LeukotrieneReceptor|Leukotriene Receptor|Sphingolipids|sphingosine kinase|Verlukast sodium|ABCC1|bronchoconstriction|ATP-binding cassette|human mast cells|CysLTR1|dyspnea



产品信息

CAS号 115103-85-0
分子式 C26H27ClN2O3S2·Na
主要靶点 LTR|Leukotriene Receptor
主要通路 G 蛋白偶联受体|免疫与炎症
分子量 537.07
纯度 98.69%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 pulmonary hypertension|RBL-2H3 cells|L 660711|LAD2|L-660711 (sodium salt)|L-660711 sodium|L-660711 sodium salt|L660711|MK 571 sodium|MK 571|MK-571 sodium salt|MK571|MK-571|MK571 sodium|MK-571 sodium|MRP1|MRP4|LeukotrieneReceptor|Leukotriene Receptor|Sphingolipids|sphingosine kinase|Verlukast sodium|ABCC1|bronchoconstriction|ATP-binding cassette|human mast cells|CysLTR1|dyspnea

靶点活性

LTD4:0.22 nM (Ki, In guinea pig lung)|LTD4:2.1 nM (Ki, In human lung)

体内活性

在类肺部,MK-571可抑制[3H]LTD4的结合(Ki:2.1±1.8 nM,n=29),而在豚鼠肺中的Ki值为0.22±0.15 nM (n=35)。但其对[3H]LTC4的结合活性较低或没有活性(IC50:32 μM,n=1,人;23±11 μM,n=16,豚鼠)。

体外活性

MK-571在健康年轻人体内耐受性良好.口服可被迅速吸收,血药浓度在给药后1.1-1.5 h后达峰.

溶解度

H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:25.78 mg/mL (48 mM);Ethanol:Insoluble

细胞实验

Cells were seeded onto 96 well plates at a concentration of 1×103 cells per well and incubated for 72 h at 37?C and 5% CO2 to allow MRP1 messenger RNA suppression to occur. Cells were then treated with either control media or one of three chemotherapy drugs temozolomide (150 µM), vincristine (100 nM), or etoposide (2 µM). Cells were then returned to the incubator for a further 72 h; after which time, Metylthiazol Tetrazolium (MTT) powder in PBS (50µl of 5 mg/ml) was added to each well. Cells were then incubated for a further 4 h after which all solution was removed and dimethyl sulfoxide (DMSO) was added. After 10 min incubation time at 37?C, absorbance was recorded at 570 nm wavelength and data was recorded and analyzed. Small molecule inhibitors MK571 (25 µM) and Reversan (15µM) were added 7 h prior to carrying out further drug treatment (temozolomide, vincristine or etoposide) or assay assessment (media change for proliferation and 2D-migration assays) (Only for Reference)

参考文献

1.Jones TR, et al. Can J Physiol Pharmacol. 1989, 67(1):17-28.
2.Amanda Tivnan, et al. Front Neurosci. 2015, 9:218.
3.Depré M, et al. Eur J Clin Pharmacol. 1992, 43(4):427-30.
4.Luo FR, et al. Drug Metab Dispos. 2002, 30(7):763-70.

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