Losartan Potassium (DuP 753)

For research use only. Not for use in humans.

目录号:S1359 别名: MK 954 中文名称:氯沙坦钾

Losartan Potassium (DuP 753) Chemical Structure

CAS No. 124750-99-8

Losartan Potassium (DuP 753, MK 954)是一种血管紧张素II受体拮抗剂,与血管紧张素II竞争性结合AT1受体,IC50为20 nM。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1060.78 现货
RMB 794.16 现货
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客户使用Selleck生产的Losartan Potassium (DuP 753)发表文献9篇:

客户使用该产品的3个实验数据:

  • Efficacy of ARBs at preventing StAR upregulation in SII-stimulated H295R cells. (A,B) Western blotting for StAR protein levels in H295R cells transfected to overexpress barr1 and treated for 6 hrs with 10 μM SII alone (SII) or in the presence of 10 μM of each of the sartans tested. Representative blots of 3 independent experiments are shown in (A), including blots for barr1 to confirm its overexpression and for GAPDH (glyceraldehyde 3-phosphate dehydrogenase) as loading control, and the StAR protein induction (as % of the SII response), as derived by densitometric quantification, is shown in (B). *, p<0.05, n=3 independent experiments/treatment. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). (C,D) Western blotting for StAR protein levels in dominant negative barr1 mutanttransfected H295R cells and treated as in (A-B). Representative blots are shown in (C), including blots for the dominant negative barr1 mutant to confirm its overexpression and for GAPDH as loading control, and the StAR protein induction (as % of vehicle-no stimulation), as derived by densitometric quantification, is shown in (D). No significant differences were observed among treatments, nor did any treatment cause any induction in StAR levels. Blots shown have been cropped to fit space requirements and run under the same experimental conditions (same gel) (the full length blots are shown in Supplementary Information). n=3 independent experiments/treatment. LOS: Losartan-; VAL: Valsartan; CAN: Candesartan; OLM: Olmesartan; IRB: Irbesartan.

    Sci Rep, 2015, 5:8116.. Losartan Potassium (DuP 753) purchased from Selleck.

    Losartan attenuates the inhibitory effect of METH on SH-SY5Y cell proliferation accompanied with decreased D3R expression. (A) Losartan attenuated the proliferation inhibitory effect of METH on SH-SY5Y cells. n = 3 for each group. Saline, **p < 0.01; 2 mM METH, ##p < 0.01, ###p < 0.001. (B) The DRs and DAT expressions were measured in SH-SY5Y cells with or without losartan treatment. Student’s t test, **p < 0.01, ***p < 0.001, n = 6 for each group. (C) The decreased D3R level was attenuated by losartan in METH-treated SH-SY5Y cells. One-way ANOVA followed by Tukey’s post-tests were performed, **p < 0.01, ***p < 0.001, n = 4 for each group

    Neurotherapeutics, 2018, 15(2):500-510. Losartan Potassium (DuP 753) purchased from Selleck.

  • Representative Trichrome II Blue staining of heart tissue sections of mice from the sham, TAC, TAC + gallic acid, TAC + losartan, TAC + carvedilol, and TAC + furosemide groups. Blue staining indicates collagen deposition. Scale bar = 100 µm

    Sci Rep, 2018, 8(1):9302. Losartan Potassium (DuP 753) purchased from Selleck.

产品安全说明书

Angiotensin Receptor抑制剂选择性比较

生物活性

产品描述 Losartan Potassium (DuP 753, MK 954)是一种血管紧张素II受体拮抗剂,与血管紧张素II竞争性结合AT1受体,IC50为20 nM。
特性 Losartan处于Ⅲ期临床试验,用于肺动脉高压的患者。
靶点
AT1 receptor [1]
20 nM
体内研究 在患有由饮食引起的高胆固醇血症的猴子体内,Losartan(180毫克/天)会引起血浆中血管紧张素Ⅱ和血管紧张素-(1-7)的明显增高。在患有由饮食引起的高胆固醇血症的猴子体内,Losartan(180毫克/天)会减少主动脉,冠状动脉和颈动脉中大约50%的脂肪纹范围。在患有由饮食引起的高胆固醇血症的猴子体内,Losartan降低低密度脂蛋白在体外氧化的敏感性,单核细胞趋化蛋白-1的血清水平,以及循环单核细胞CD11b的表达。[2]在怀孕的Fbn1C1039G/+小鼠的主动脉培养基中, Losartan (0.6 克/升饮用水)防止弹性纤维碎裂和迟钝的TGF-β信号,由减少的pSmad2核积累所证明。在怀孕的Fbn1C1039G/+小鼠体内,Losartan (0.6 克/升饮用水)使末梢空间管径减少。在怀孕的Fbn1C1039G/+小鼠体内,Losartan (0.6 克/升饮用水)改善肺部疾病的临床表现,这无法合理的与改善的血流动力学相关联。[3]载脂蛋白E不足的小鼠体内,Losartan(5 毫克/千克/天) 导致动脉粥样硬化病变的发展显著下降。载脂蛋白E不足的小鼠体内, Losartan(5 毫克/千克/天) 在CuSO4存在下进行培养后,显著降低小鼠低密度脂蛋白对脂肪氧化的敏感性。[4]在雄性Sprague Dawley大鼠体内,Losartan (10 毫克/千克)给药增加4倍到6倍的血管紧张素水平,而不改变血液BK水平。在雄性Sprague Dawley大鼠体内,Losartan (10 毫克/千克)增加100倍血浆肾素水平,血浆血管紧张素水平减少到对照组的24%,而不改变血浆醛固醇水平。[5]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验:[2]
- 合并
  • Animal Models: Male cynomolgus monkeys fed a diet containing 0.067 mg cholesterol/kJ
  • Dosages: 180 mg/d
  • Administration: Dietary
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 92 mg/mL (199.12 mM)
Water 92 mg/mL (199.12 mM)
Ethanol 92 mg/mL (199.12 mM)
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
Saline
30 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 462.01
化学式

C22H23ClKN6O

CAS号 124750-99-8
储存条件 粉状
溶于溶剂
别名 MK 954

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

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 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

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 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00880386 Withdrawn Drug: Losartan Dyspnea|Lung Cancer|Pulmonary Complications|Radiation Fibrosis University of South Florida|National Cancer Institute (NCI) March 2009 Not Applicable

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操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID