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  1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. Bisoprolol

Bisoprolol  (Synonyms: 比索洛爾)

目錄號(hào): HY-129029 純度: 99.78%
COA 產(chǎn)品使用指南

Bisoprolol 是一種有效的、選擇性的、具有口服活性的 β1 腎上腺素受體 (β1-adrenergic receptor) 阻滯劑,對(duì) β2 受體的活性很小。Bisoprolol 可用于高血壓,冠狀動(dòng)脈疾病和穩(wěn)定的心室功能障礙的研究。

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Bisoprolol Chemical Structure

Bisoprolol Chemical Structure

CAS No. : 66722-44-9

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Customer Review

Other Forms of Bisoprolol:

    Bisoprolol purchased from MCE. Usage Cited in: Mol Neurobiol. 2019 Jan;56(1):367-377.  [Abstract]

    Inhibitory effect of bisoprolol fumarate on PrPSc accumulation in N2a-FK cells. After the cells are incubated in medium mixed with each concentration of sample compound or water (negative control) for 48 h, the collected cell lysates are digested with proteinase K. Western blotting is then performed for quantification of the PrPSc level.

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

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research[1][2].

    IC50 & Target[1]

    Beta-1 adrenergic receptor

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A-375 IC50
    > 100 μM
    Compound: Bisoprolol
    Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    [PMID: 32216987]
    SK-MEL-28 IC50
    > 100 μM
    Compound: Bisoprolol
    Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    [PMID: 32216987]
    SK-MEL-5 IC50
    > 100 μM
    Compound: Bisoprolol
    Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    [PMID: 32216987]
    體外研究
    (In Vitro)

    Bisoprolol (2 μM, 1 h) protects myocardial cells (H9c2) from ischemia/reperfusion (I/R) injury[2].
    Bisoprolol (2 μM, 1 h) reduces the H/R-induced ROS production and apoptosis in H9c2 cells[2].
    Bisoprolol (2 μM, 1 h) increases AKT and GSK3β phosphorylation in H9c2 cells[2].
    Bisoprolol (100 μM, 24 h) reverses Epinephrine-inhibited emigration in cholesterol-loaded DCs (dendritic cell) through increasing in β-arrestin 2, CCR7 and PI3K phosphorylation[3].

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

    Cell Viability Assay[2]

    Cell Line: H9c2 cells
    Concentration: 0.2, 2, 20 μM
    Incubation Time: 1 h
    Result: Elevated the survival rates of cardiomyocytes subjected to H/R (hypoxia/reoxygenation) to 73.20%, 90.38%, 81.25% respectively.

    Cell Migration Assay [3]

    Cell Line: DCs
    Concentration: 100 μM
    Incubation Time: 6, 12, 24 h
    Result: Increased the amount of migrating cells by 46.00% (6 h), 64.25% (12 h) and 55.74% (24 h).
    體內(nèi)研究
    (In Vivo)

    Bisoprolol (oral administration, 5 mg/kg, for 1 week) increases left ventricular ejection fraction (LVEF) and decreases the heart rate value[2].
    Bisoprolol (oral gavage, 8 mg/kg, daily for four weeks) shows protective effects against Cadmium-induced myocardial toxicity in rats[4].
    Bisoprolol (oral gavage, 1 mg/kg, daily for 6 weeks) reverses small conductance calcium-activated potassium channel (SK) remodeling in a volume-overload rat model[5].

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

    Animal Model: Ischemia/reperfusion (I/R) injury rats[2]
    Dosage: 0.5, 5, 10 mg/kg
    Administration: Oral administration, for 1 week, prior to 0.5 h ischemia/4 h reperfusion.
    Result: Reduced infarct size from 44% in I/R group to 31% in treated group.
    Animal Model: Cadmium-induced rats[4]
    Dosage: 2, 8 mg/kg
    Administration: Oral gavage, daily for four weeks.
    Result: Decreased mean arterial pressure (MAP) at 8 mg/kg.
    Decreased serum biomarkers (ALT, AST) and NF-kB p65 expression and TNF-α levels (cardiac tissue samples) at 8 mg/kg.
    Clinical Trial
    分子量

    325.44

    Formula

    C18H31NO4

    CAS 號(hào)
    性狀

    液體(密度:1.033±0.06 g/cm3

    顏色

    Colorless to light yellow

    中文名稱

    比索洛爾

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲(chǔ)存方式
    Pure form -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    DMSO 中的溶解度 : 350 mg/mL (1075.47 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 3.0728 mL 15.3638 mL 30.7276 mL
    5 mM 0.6146 mL 3.0728 mL 6.1455 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)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(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    純度 & 產(chǎn)品資料
    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.0728 mL 15.3638 mL 30.7276 mL 76.8191 mL
    5 mM 0.6146 mL 3.0728 mL 6.1455 mL 15.3638 mL
    10 mM 0.3073 mL 1.5364 mL 3.0728 mL 7.6819 mL
    15 mM 0.2049 mL 1.0243 mL 2.0485 mL 5.1213 mL
    20 mM 0.1536 mL 0.7682 mL 1.5364 mL 3.8410 mL
    25 mM 0.1229 mL 0.6146 mL 1.2291 mL 3.0728 mL
    30 mM 0.1024 mL 0.5121 mL 1.0243 mL 2.5606 mL
    40 mM 0.0768 mL 0.3841 mL 0.7682 mL 1.9205 mL
    50 mM 0.0615 mL 0.3073 mL 0.6146 mL 1.5364 mL
    60 mM 0.0512 mL 0.2561 mL 0.5121 mL 1.2803 mL
    80 mM 0.0384 mL 0.1920 mL 0.3841 mL 0.9602 mL
    100 mM 0.0307 mL 0.1536 mL 0.3073 mL 0.7682 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    產(chǎn)品名稱:
    Bisoprolol
    目錄號(hào):
    HY-129029
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