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  1. GPCR/G Protein
  2. Angiotensin Receptor
  3. Losartan potassium

Losartan potassium  (Synonyms: 氯沙坦鉀; DuP-753 potassium)

目錄號: HY-17512A 純度: 99.91%
COA 產(chǎn)品使用指南

Losartan potassium (DuP-753 potassium) 是血管緊張素 II 受體 1 型 (AT1)拮抗劑,與血管緊張素 II 與 AT1 的結合競爭,IC50 為 20 nM。

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Losartan potassium Chemical Structure

Losartan potassium Chemical Structure

CAS No. : 124750-99-8

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10 mM * 1 mL in DMSO ¥500
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500 mg ¥400
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1 g ¥500
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5 g ¥1200
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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 34 篇科研文獻

WB

    Losartan potassium purchased from MCE. Usage Cited in: FASEB J. 2018 Sep;32(9):5051-5062.  [Abstract]

    HUVECs are starved for 12 h, treated with 10 mg/mL (9.56 μM) of AngII with or without Losartan or PD123319 for 12 h, and are subsequently used for Western blot analysis.

    查看 Angiotensin Receptor 亞型特異性產(chǎn)品:

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    Losartan potassium (DuP-753 potassium) is an angiotensin II receptor type 1 (AT1) antagonist, competing with the binding of angiotensin II to AT1 with an IC50 of 20 nM.

    IC50 & Target

    AT1 Receptor

     

    體外研究
    (In Vitro)

    Losartan potassium 競爭血管緊張素 II 與 AT1 受體的結合。抑制 50% 血管緊張素 II 結合的濃度 (IC50) 為 20 nM[1]。Losartan potassium (40 μM) 影響 ISC 但阻止 ANGII 對 ISC 的影響[2]。Losartan potassium 顯著降低子宮內膜癌細胞中 Ang II 介導的細胞增殖。與單獨使用每種藥物相比,Losartan potassium 和抗 miR-155 的組合具有顯著更強的抗增殖作用[3]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    體內研究
    (In Vivo)

    Losartan potassium (0.6 g/L,po) 處理的 Fbn1C1039G/+ 小鼠顯示相對于安慰劑處理的 Fbn1C1039G 遠端空域口徑減少/+ 。滴定 Losartan potassium 和普萘洛爾的劑量以達到可比較的血液動力學效果。pSmad2 核染色分析表明,Losartan potassium 拮抗 Fbn1C1039G/+ 小鼠主動脈壁中的 TGF-β 信號傳導。Losartan potassium 可以改善肺部的疾病表現(xiàn),這一事件與改善的血流動力學似乎無關[4]。Losartan potassium (10 mg/kg,動脈內注射) 使血液血管緊張素水平增加四到六倍。Losartan potassium (10 mg/kg,ip) 使血漿腎素水平增加 100 倍;血漿血管緊張素原水平降至對照的 24%;和血漿醛固酮水平?jīng)]有變化[5]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    461.00

    Formula

    C22H22ClKN6O

    CAS 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    氯沙坦鉀

    運輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    溶解性數(shù)據(jù)
    細胞實驗: 

    DMSO 中的溶解度 : ≥ 110 mg/mL (238.61 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

    H2O 中的溶解度 : 50 mg/mL (108.46 mM; 超聲助溶)

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質量 1 mg 5 mg 10 mg
    1 mM 2.1692 mL 10.8460 mL 21.6920 mL
    5 mM 0.4338 mL 2.1692 mL 4.3384 mL
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C儲存時,請在1年內使用, -20°C儲存時,請在6個月內使用。

    * 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

    • 摩爾計算器

    • 稀釋計算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗:

    以下溶解方案,請直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比; 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請依序添加每種溶劑: PBS

      Solubility: 100 mg/mL (216.92 mM); 澄清溶液; 超聲助溶

    動物溶解方案計算器
    請輸入動物實驗的基本信息:

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    由于實驗過程有損耗,建議您多配一只動物的量
    計算結果
    工作液所需濃度 : mg/mL
    該產(chǎn)品水溶性佳,請具體參考實測 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,如有需要,請與 MCE 中國技術支持聯(lián)系。
    純度 & 產(chǎn)品資料

    純度: 99.91%

    參考文獻
    Cell Assay
    [3]

    An MTT assay is used to measure cell proliferation and viability. For the assay, 5000 cells in 200?μL media per well are seeded in a 96 well plate. After overnight incubation to allow for cell attachment, the medium is removed by suction. MTT at 1?mg/mL concentration in serum-free medium is added and then incubated for 4?h at 37°C. After removal of MTT solution, 100?μL of DMSO is added to dissolve formazan crystals. Absorbance at 570?nm and at 600?nm as a reference is then measured using a microplate reader. The difference in absorbance is thus relative to the extent of cell survival.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [4]

    Female Fbn1C1039G/+ mice undergo timed matings with wild-type male mice. At 14.5d post-coitum, pregnant female Fbn1C1039G/+ mice are treated with oral losartan (0.6 g/L in drinking water; n=10), propranolol (0.5 g/L; n=6) or placebo (n=12). Therapy is continued throughout lactation and after weaning until 10 months of age. Mice are sacrificed and examined using the techniques described above. Propranolol is used for comparison with losartan because β-adrenergic receptor blockade is the current albeit controversial standard of care to modulate abnormal growth of the aortic root in MFS. Beginning at 7 weeks of age, wild-type and Fbn1C1039G/+ mice are treated with oral losartan (0.6 g/L in drinking water; n=5), propranolol (0.5 g/L; n=7) or placebo (n=10). Mice are continued on oral therapy for 6 months and then sacrificed.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    參考文獻

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C儲存時,請在1年內使用, -20°C儲存時,請在6個月內使用。

    可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.1692 mL 10.8460 mL 21.6920 mL 54.2299 mL
    5 mM 0.4338 mL 2.1692 mL 4.3384 mL 10.8460 mL
    10 mM 0.2169 mL 1.0846 mL 2.1692 mL 5.4230 mL
    15 mM 0.1446 mL 0.7231 mL 1.4461 mL 3.6153 mL
    20 mM 0.1085 mL 0.5423 mL 1.0846 mL 2.7115 mL
    25 mM 0.0868 mL 0.4338 mL 0.8677 mL 2.1692 mL
    30 mM 0.0723 mL 0.3615 mL 0.7231 mL 1.8077 mL
    40 mM 0.0542 mL 0.2711 mL 0.5423 mL 1.3557 mL
    50 mM 0.0434 mL 0.2169 mL 0.4338 mL 1.0846 mL
    60 mM 0.0362 mL 0.1808 mL 0.3615 mL 0.9038 mL
    80 mM 0.0271 mL 0.1356 mL 0.2711 mL 0.6779 mL
    100 mM 0.0217 mL 0.1085 mL 0.2169 mL 0.5423 mL

    * 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

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    產(chǎn)品名稱:
    Losartan potassium
    目錄號:
    HY-17512A
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