中文名称: | MK-571 sodium salt hydrate 促销 | ||||
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英文名称: | MK-571 sodium salt hydrate | ||||
别名: | 5-(3-(2-(7-Chloroquinolin-2-yl)ethenyl)phenyl)-8-dimethylcarbamyl-4,6-dithiaoctanoic acid sodium salt hydrate | ||||
CAS No: | 115103-85-0 | 分子式: | C26H26ClN2NaO3S2.XH2O | 分子量: | 537.07 |
CAS No: | 115103-85-0 | ||||
分子式: | C26H26ClN2NaO3S2.XH2O | ||||
分子量: | 537.07 | ||||
MDL: | MFCD11114392 |
基本信息
产品编号: |
M70020 |
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产品名称: |
MK-571 sodium salt hydrate |
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CAS: |
115103-85-0 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
6个月 |
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分子量: |
537.07 |
-20℃ |
1个月 |
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化学名: |
5-(3-(2-(7-Chloroquinolin-2-yl)ethenyl)phenyl)-8-dimethylcarbamyl-4,6-dithiaoctanoic acid sodium salt hydrate |
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Solubility (25°C): |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
1.8620mL |
9.3098mL |
18.6195mL |
5mM |
0.3724mL |
1.8620mL |
3.7239mL |
10mM |
0.1862mL |
0.9310mL |
1.8620mL |
生物活性
产品描述 |
一种有效的选择性的白细胞三烯D4LTD4)拮抗剂和ABCC多药耐药蛋白1(MRP1)抑制剂。 |
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靶点 |
LTD4 0.22nM (Ki,In guinea pig lung) |
LTD4 2.1nM (Ki,In human lung) |
体外研究 |
MK-571 (L660,711) is a potent and selective competitive inhibitor of [3H]leukotriene D4 binding in guinea pig (Ki value,0.22nM) and human (Ki value,2.1nM) lung membranes.MK-571 is essentially inactive versus [3H]LTC4 binding with IC50 values of 23±11μM (n=16) and 32μM (n=1) in guinea pig and human lung,respectively.MK-571 competitively antagonizes contractions of guinea pig trachea and ileum induced by leukotriene (LT) D4 (respective pA2 values,9.4 and 10.5) and LTE4 (respective pA2 values,9.1 and 10.4) and contractions of human trachea induced by LTD4 (pA2 value,8.5).MK-571 (58nM) antagonizes contractions of guinea pig trachea induced by LTC4 in the absence (dose ratio=28) but not in the presence of 45mM L-serine borate (dose ratio less than 2).MK-571 (19μM) does not block contractions of guinea pig trachea induced by histamine,acetylcholine,5-hydroxytryptamine,PGF2 alpha,U-44069,or PGD2.In the presence of atropine,mepyramine,and indomethacin,MK-571 (19μM) inhibits a small component of the response to antigen on guinea pig trachea but completely blocked anti-IgE-induced contractions of human trachea. |
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体内研究 |
MK-571 (L-660,711;i.v.) antagonizes bronchoconstriction induced in anesthetized guinea pigs by i.v.LTC4,LTD4,and LTE4 but does not block bronchoconstriction to arachidonic acid,U-44069,5-hydroxytryptamine,histamine, or acetylcholine.Intraduodenal MK-571 antagonizes LTD4 (0.2-12.8μg/kg)-induced bronchoconstriction in guinea pigs,and p.o.MK-571 blockes LTD4- and Ascaris-induced bronchoconstriction in conscious squirrel monkeys and ovalbumin-induced bronchoconstriction in conscious sensitized rats treated with methysergide (3μg/kg).Hypoxia-exposed WT mice are treated with either saline or MK-571 (5mg/kg/d or 25mg/kg/d) for 2 more weeks while being maintain in hypoxic conditions.Saline-treated mice display all the hallmarks of PH (i.e.,an increase in RVSP,Fulton index,and arterial wall thickness).However,following hypoxia,MK-571-treated mice display lower RVSP and Fulton index and a decrease in the medial thickening of small pulmonary arteries and arterioles. |
推荐实验方法(仅供参考)
动物实验: |
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Mice The Mrp4-/- mice are used. Concerning the PH reversal study,5-week-old WT mice are maintained in hypoxia for 3 weeks,then are randomized to receive,for 2 weeks,oral vehicle or MK-571 at the doses of either 5mg/kg/d or 25mg/kg/d.At the same time, the experiment is designed for mice in normoxia conditions.Increased hematocrit valuesare checked to assess the efficiency of hypoxia. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )