1. Vitamin D Related/Nuclear Receptor
  2. VD/VDR
  3. Seocalcitol

Seocalcitol  (Synonyms: 西奥骨化醇; EB 1089)

目录号: HY-32341 纯度: 99.51%
COA 产品使用指南

Seocalcitol 是一种 vitamin D 类似物,作用于人骨肉瘤 MG-63 细胞,结合 vitamin D 受体蛋白,Kd 为 0.27 nM。

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Seocalcitol Chemical Structure

Seocalcitol Chemical Structure

CAS No. : 134404-52-7

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5 mg ¥4440
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10 mg ¥7040
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Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

WB

    Seocalcitol purchased from MCE. Usage Cited in: Oncotarget. 2016 Sep 20;7(38):62240-62254.  [Abstract]

    P-RPS levels in cells incubated with various prostate cancer cell inhibitors. A. PC3, B. C4-2B. DPT: deoxypodophyllotoxin; EB1089(EB; 1,25-vitamin D3 analog); T0901317, LXR agonist.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Seocalcitol is a vitamin D analog, binds vitamin D receptor protein from human osteosarcoma MG-63 cells with Kd of 0.27 nM.

    IC50 & Target

    Kd: 0.27 nM (vitamin D receptor)[1]

    体外研究
    (In Vitro)

    Seocalcitol (EB 1089) 是小鼠骨髓培养物中破骨细胞募集的刺激剂,EC50 为 0.1 nM。Seocalcitol 刺激骨吸收,估计 EC50 为 0.03 nM[1]。Seocalcitol (EB 1089) 在肾脏中引起 24-羟化酶 mRNA 的剂量依赖性诱导 (EC50=0.4±0.13)。在肾脏中,Seocalcitol 的 Kd 值为 0.48±0.04 nM。然而,在肠道中,Seocalcitol 的 Kd 为 1.43±0.19 nM)[2]。Seocalcitol (0.1-10 nM) 以剂量依赖的方式诱导细胞分化。观察到 1 nM Seocalcitol (EB 1089) 比 1 nM VD3 具有更高的分化活性。

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

    体内研究
    (In Vivo)

    Seocalcitol (EB1089) 是一种合成的维生素 D 类似物,相对于 1,25 (OH) 2VD3 表现出降低的高血钙活性。在另一项研究中,每隔一天以 0.5 μg/kg 体重的剂量对 C3H/Sy 小鼠长期腹腔内 (IP) 给药 Seocalcitol 对肝细胞癌 (HCC) 的发展具有非常强的抑制作用[4]。Seocalcitol (EB 1089) 以 0.38 或 1.25 μg/kg 体重 (BW)/天的剂量腹膜内注射,每天给药于 4 至 12 日龄 (P4 至 P12) 的产后大鼠。当单独使用或与地塞米松、全反式维甲酸 (RA) 或维甲酸联合使用时,只有最高剂量的司 Seocalcitol (1.25 μg/kg BW) 会显著降低体重增加[5]

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

    Clinical Trial
    分子量

    454.68

    Formula

    C30H46O3

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    西奥骨化醇

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, protect from light, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 50 mg/mL (109.97 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 2.1993 mL 10.9967 mL 21.9935 mL
    5 mM 0.4399 mL 2.1993 mL 4.3987 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1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    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.50 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。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.50 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,此方案实验周期在半个月以上的动物实验酌情使用。

      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玉米油中,混合均匀。

    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)。

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    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: 99.51%

    参考文献
    Kinase Assay
    [1]

    Vitamin D receptor protein is prepared from cultures of human osteosarcoma cell line MG-63. Suspensions of 5×107 cells/mL are homogenized, sonicated, and centrifuged at 30,000g for 1 h at 4°C. The presence of the 1α,25(OH)2D3 receptor is verified by sucrose density gradient analysis. The supernatants are adjusted to 2 mg protein/mL and used for binding studies. Samples of 500 μL are incubated with 10,000 dpm [3H]1α,25(OH)2D3 (180 Ci/mmol) and increasing concentrations of 1α,25(OH)2D3 or vitamin D3 analogs are added. After incubation for 60 min at 22°C, bound and free [3H]1α,25(OH)2D3 are separated on dextran-coated charcoal. Each compound is tested in three separate experiments[1].

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

    Cell Assay
    [3]

    This fluorescent dye allowed to determine ROS release in HL60 cells, untreated or treated VD3 or Seocalcitol. Briefly, after treatment, HL60 cells are washed and re-suspended at 106 cells/mL in RPMI-1640 without FCS and phenol red. Then, 10 μM H2-DCFDA probe is added to each plate at a final volume of 2 mL. Cells are incubated for 45 min at 37°C in the dark. A second wash is made before the fluorescence analysis using spectrometer at 488 nm intensity excitation λex and 516 nm emission λem. Results, in arbitrary fluorescence units (AFU), are expressed according to the ratio [(AFU-treated cells)/(AFU control cells)]×100[3].

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

    Animal Administration
    [4][5]

    Mice[4]
    Six- to eight-week-old male BALB/c NU/Nu mice are inoculated subcutaneously with 106 SKHEP-1 cells into the right flank. Twenty-four hours after inoculation, mice are randomly assigned to a control group (n=10) or the treatment groups (n=10), receiving 0.02, 0.1 or 0.5 μg/kg per day of Seocalcitol (intraperitoneal or oral on alternate days). Control animals receive propylene glycol alone. Tumor size is measured using vernier calipers every third day and the volumes are estimated using the formula 0.5×length×(width)2. Animals receive sterile food and water.
    Rats[5]
    Newborn Sprague-Dawley rat pups are randomly assigned to 1 of 6 treatment groups, consisting of daily intraperitoneal injections of the vitamin D analogue Seocalcitol (0.38 or 1.25 μg/kg body weight) alone, or in combination with all-trans retinoic acid (RA; 500 μg/kg body weight) and/or Dexamethasone (DEX; 0.25 μg/day) in a 3×2×2 factorial design. Seocalcitol and RA injections are conducted on P3 through P12, whereas Dexamethasone is administered on P4 through P12. Seocalcitol is prepared for injections in a quantity sufficient for all injections by dilution from a stock solution (4 mM in isopropanol) into the carrier Solutol HS 15 (BASF). Solutol-diluted Seocalcitol is stored as aliquots in sealed glass vials under nitrogen gas at 4°C, with daily injections conducted with freshly unsealed aliquots of Seocalcitol. Stock solutions of RA (50 mg/mL DMSO are stored under nitrogen at −80°C and prepared for injection by dilution of freshly thawed aliquots into cottonseed oil (2 μg/μL). A Dexamethasone stock solution (10 mg/mL ethanol) is stored under nitrogen at 4°C and prepared fresh for daily injections in 0.9% NaCl (0.25 μg/μL). All rats receive equivalent volumes of the 3 carrier solutions employed (solutol, cottonseed oil, 0.9% NaCl). Seocalcitol and RA are administered as a 2-phase solution via a 10 μL injection using a 20 μL glass-barreled syringe and a 28-gauge needle, whereas Dexamethasone is administered in a separate 10 μL injection.

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

    参考文献

    Seocalcitol 相关分类

    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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1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 2.1993 mL 10.9967 mL 21.9935 mL 54.9837 mL
    5 mM 0.4399 mL 2.1993 mL 4.3987 mL 10.9967 mL
    10 mM 0.2199 mL 1.0997 mL 2.1993 mL 5.4984 mL
    15 mM 0.1466 mL 0.7331 mL 1.4662 mL 3.6656 mL
    20 mM 0.1100 mL 0.5498 mL 1.0997 mL 2.7492 mL
    25 mM 0.0880 mL 0.4399 mL 0.8797 mL 2.1993 mL
    30 mM 0.0733 mL 0.3666 mL 0.7331 mL 1.8328 mL
    40 mM 0.0550 mL 0.2749 mL 0.5498 mL 1.3746 mL
    50 mM 0.0440 mL 0.2199 mL 0.4399 mL 1.0997 mL
    60 mM 0.0367 mL 0.1833 mL 0.3666 mL 0.9164 mL
    80 mM 0.0275 mL 0.1375 mL 0.2749 mL 0.6873 mL
    100 mM 0.0220 mL 0.1100 mL 0.2199 mL 0.5498 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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