1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Apoptosis Anti-infection
  2. Histamine Receptor Apoptosis Parasite HBV
  3. Osthole

Osthole  (Synonyms: 蛇床子素; Osthol; NSC 31868)

目录号: HY-N0054 纯度: 99.95%
COA 产品使用指南

Osthole (Osthol) 是一种天然抗组胺药替代试剂。Osthole 可有效抑制组胺 H1 受体 (histamine H1 receptor) 活性。Osthole 还可抑制细胞培养物中 HBV 的分泌。

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Osthole Chemical Structure

Osthole Chemical Structure

CAS No. : 484-12-8

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10 mM * 1 mL in DMSO ¥500
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250 mg ¥410
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1 g ¥1190
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5 g ¥3500
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Other Forms of Osthole:

    Osthole purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2019 May;40(5):608-619.  [Abstract]

    Osthole reduces the TMX-induced inflammatory response. Mice are intraperitoneally injected with Osthole (100 mg/kg).

    Osthole purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2019 May;40(5):608-619.  [Abstract]

    Osthole reduces the TMX-induced inflammatory response. Mice are intraperitoneally injected with Osthole (100 mg/kg)

    Osthole purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2019 May;40(5):608-619.  [Abstract]

    Osthole significantly increases the expression of antioxidant genes (GPX1, SOD2). Mice are intraperitoneally injected with osthole (100 mg/kg).

    Osthole purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2019 May;40(5):608-619.  [Abstract]

    Osthole significantly increases the expression of antioxidant genes (GCL-c, and G6pdh. Mice are intraperitoneally injected with osthole (100 mg/kg).

    Osthole purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2019 May;40(5):608-619.  [Abstract]

    Mice are intraperitoneally injected with Osthole (100 mg/kg). After 24h, TMX (90mg/kg) is administered to mice. Mice are sacrificed 8 h after the TMX injections. Western blot analyses of the liver homogenates are performed.

    Osthole purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2019 May;40(5):608-619.  [Abstract]

    Osthole significantly suppresses the expression of pro-oxidant genes (NOX2 and ACOX). Mice are intraperitoneally injected with osthole (100 mg/kg).

    Osthole purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2019 May;40(5):608-619.  [Abstract]

    Osthole reduces TMX-induced oxidative stress.

    Osthole purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2018 Jan;39(1):74-84.  [Abstract]

    Osthole inhibits the metabolic activation of APAP and promotes APAP clearance. Hepatic SULT2A1 and UGT1A1 levels are determined by Western blotting.

    Osthole purchased from MCE. Usage Cited in: Front Physiol. 2018 Nov 21;9:1650.  [Abstract]

    Western blot analyses (E) of PCNA, cyclin D1 and p21 cip1 in the treatment of FBS and OST.

    Osthole purchased from MCE. Usage Cited in: Front Physiol. 2018 Nov 21;9:1650.  [Abstract]

    Representative micrographs of immunofluorescent staining of FN (red) and a-SMA (green) with the treatment of TGFβ1 and OST.

    Osthole purchased from MCE. Usage Cited in: Front Physiol. 2018 Nov 21;9:1650.  [Abstract]

    OST suppress activation of NRK-49F cells. NRK-49F are preincubated with OST for 30 min before TGFβ1 (5 ng/ml) and are harvested 24 h after TGFb1 stimulation. Western blot analyses of a-SMA, Col I (collagen I) and FN (fibronectin) are showed.

    Osthole purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2017 Aug;38(8):1120-1128.  [Abstract]

    Osthole attenuates the phosphorylation of p38 in TNBS-induced colitis. Mice receive Osthole intraperitoneally at 100 mg/kg once daily starting at three days before being exposed to TNBS treatments and until the end of the experiments. Colitis is induced by infusing a 100 μL enema of TNBS (2.8 mg) in 50% ethanol into the colonic lumen. Western blot analysis of the colonic mucosa homogenates is performed 2 d after the initial rectal TNBS administration.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Osthole (Osthol) is a natural antihistamine alternative. Osthole may be a potential inhibitor of histamine H1 receptor activity. Osthole also suppresses the secretion of HBV in cells.

    IC50 & Target

    Histamine H1 receptor[1]

    体外研究
    (In Vitro)

    Osthole (p<0.0001) 和 Fexofenadine (p<0.001) 抑制研究组中组胺诱导的 HRH-1 mRNA 表达增加。在用组胺/ Osthole 培养的细胞中也观察到了这一结果;其中与组胺相比,组合物质降低了 HRH-1 mRNA 表达 (p<0.0001)[1]
    当 Osthole 以高达 100 μM 的剂量使用时,细胞活力评估未检测到明显的毒性。然而,当剂量达到 500 μM 时,Osthole 开始表现出毒性作用。基于这些观察,Osthole 用于所有体外研究,剂量范围为 10 至 100 μM。Osthole 剂量依赖性地促进成骨细胞分化,如 I 型胶原 (col1)、骨唾液蛋白 (BSP) 和骨钙素 (OC) (培养 2 天)。Osthole 以剂量依赖的方式促进小鼠原代成骨细胞的 ALP 活性[2]

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

    体内研究
    (In Vivo)

    将 Osthole 以每天 5 mg/kg 的剂量皮下注射到小鼠颅骨上可显著刺激局部骨形成 (对最后一次注射后 2 周采集的颅骨样本进行组织学分析所示,并用 H&E orange G 染色)。组织形态学分析显示 Osthole对骨形成有显著影响,与阳性对照微管抑制剂 TN-16 一样有效。然而,当以每天 1 mg/kg 的剂量使用 Osthole 时,看不到这种效果。腹膜内注射 Osthole 8 周可显著逆转去卵巢大鼠的骨质流失。用三硝基苯酚一品红染色的 L4 样本的组织学检查表明,用 Osthole 处理的去势大鼠的小梁结构部分恢复。组织形态学分析表明,Osthole 处理可显著增加总 BMD、骨小梁体积和骨小梁厚度,并减少骨小梁分离[2]

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

    分子量

    244.29

    Formula

    C15H16O3

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    蛇床子素;蛇床籽素;欧芹酚甲醚

    结构分类
    初始来源
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 100 mg/mL (409.35 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 4.0935 mL 20.4675 mL 40.9350 mL
    5 mM 0.8187 mL 4.0935 mL 8.1870 mL
    查看完整储备液配制表

    * 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
    储备液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (10.23 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (10.23 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.95%

    参考文献
    Cell Assay
    [1]

    Peripheral blood samples are collected from participants between 7.00 and 9.00 a.m. on the first study day and these are concentrated in grouping tubes with K3EDTA. Fresh PBMCs are then prepared. Isolated cells are seeded on 24-well plates at 1×106 per well with RPMI-1640 and supplemented with 1% heat inactivated human AB serum, 1% gentamicin and 0.25% PHA. Active reagents are added to each well after 24 h and pure medium formed the control for each substance. Cells are then harvested after a further three days[1].

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

    Animal Administration
    [2]

    Mice[2]
    Four-week-old ICR Swiss mice are injected subcutaneously over the calvarial surface with or without the treatment of Osthole twice a day for 5 consecutive days at the doses of 1 and 5 mg/kg per day (3 mice per group). Microtubule inhibitor TN-16 is used as a positive control (5 mg/kg per day, by subcutaneous injection, twice a day for 2 days; 3 mice per group). All mice are euthanized 3 weeks after treatment, and calvariae are dissected, fixed in 10% phosphate-buffered formalin for 2 days, decalcified in 10% EDTA for 2 weeks, and embedded in paraffin. Histologic sections are cut and stained with hematoxylin and eosine orange G. New bone area over the calvarial surface is quantified by histomorphometry using the OsteoMeasure System. To measure mineral appositional rate (MAR) and bone-formation rate (BFR), double calcein labeling is performed at days 7 and 14 by intraperitoneal injection (20 mg/kg), and mice are euthanized 7 days after the second labeling. The labeling is examined in plastic sections. The dissected calvarial samples are fixed in 75% ethanol and embedded in methyl methacrylate. Unstained transverse sections (3 µm thick) are examined with a fluorescent microscope. MAR and BFR are measured using the OsteoMeasure System.
    Rats[2]
    Thirty 6-month-old female Sprague-Dawley rats are used. After anesthesia with intraperitoneal nembutal injection (30 mg/kg), the rats are randomized by body weight into three groups for the surgery (n=10/group): group 1: sham surgery followed by PBS vehicle treatment (sham+VEH); group 2: ovariectomy followed by vehicle treatment (OVX+VEH); and group 3: ovariectomy followed by Osthole treatment (OVX+OST). The treatment is started 1 month after surgery and continued for 8 weeks. Vehicle or Osthole (100 mg/kg per day) is administered orally once a day for 8 weeks. Before rats are euthanized at the end of the experiments, the total bone mineral density (BMD, g/m2) is measured using dual-energy X-ray absorptiometry. The fourth lumbar vertebrae (L4) then are dissected for histomorphometric and micro-computed tomographic (µCT) analysis, and the left femoral shafts are used for biomechanical testing.

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

    参考文献

    完整储备液配制表

    * 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
    储备液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 4.0935 mL 20.4675 mL 40.9350 mL 102.3374 mL
    5 mM 0.8187 mL 4.0935 mL 8.1870 mL 20.4675 mL
    10 mM 0.4093 mL 2.0467 mL 4.0935 mL 10.2337 mL
    15 mM 0.2729 mL 1.3645 mL 2.7290 mL 6.8225 mL
    20 mM 0.2047 mL 1.0234 mL 2.0467 mL 5.1169 mL
    25 mM 0.1637 mL 0.8187 mL 1.6374 mL 4.0935 mL
    30 mM 0.1364 mL 0.6822 mL 1.3645 mL 3.4112 mL
    40 mM 0.1023 mL 0.5117 mL 1.0234 mL 2.5584 mL
    50 mM 0.0819 mL 0.4093 mL 0.8187 mL 2.0467 mL
    60 mM 0.0682 mL 0.3411 mL 0.6822 mL 1.7056 mL
    80 mM 0.0512 mL 0.2558 mL 0.5117 mL 1.2792 mL
    100 mM 0.0409 mL 0.2047 mL 0.4093 mL 1.0234 mL
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    • 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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    目录号:
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