2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Autophagy
  3. RAR/RXR Cytochrome P450 Autophagy
  4. Talarozole

Talarozole  (Synonyms: 他拉罗唑; R115866)

目录号: HY-14531 纯度: 99.61%
COA 产品使用指南

摩尔计算器

Talarozole (R115866) 是一种口服性全反式维甲酸代谢阻断剂 (RAMBA)，可提高内源性全反式维甲酸 (RA) 的细胞内水平。Talarozole 抑制 CYP26A1 和 CYP26B1，IC50 值分别为 5.4 和 0.46 nM。

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Talarozole Chemical Structure

Talarozole Chemical Structure

CAS No. : 201410-53-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1430
In-stock
2 mg ￥900
In-stock
5 mg ￥1300
In-stock
10 mg ￥1800
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50 mg ￥4200
In-stock
100 mg ￥5900
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200 mg   询价  
500 mg   询价  

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Customer Review

Other Forms of Talarozole:

Talarozole 相关抗体

Top Publications Citing Use of Products

    Talarozole purchased from MCE. Usage Cited in: PLoS Genet. 2017 Dec 11;13(12):e1007112.  [Abstract]

    Embryos raised in media containing 0.01% DMSO develop normally. 100% of embryos treated with Talarozole between 54 and 60 hpf displayed ectopic muscle projection in the second pharyngeal arch, and the intermandibularis posterior muscles overextended in 58.3% of embryos (n=64).

    Talarozole purchased from MCE. Usage Cited in: J Exp Zool B Mol Dev Evol. 2017 Sep;328(6):575-586.  [Abstract]

    Effect of R115866 on COL9A1 expression. R115866 enhances the effect of ATRA on COL9A1 expression. R115866 (1 μM) is dissolved in DMSO. Control receive the vehicle only.

    Talarozole purchased from MCE. Usage Cited in: University of Texas. August 2017.

    100% of embryos treated with Talarozole between 54 and 60 hpf displayed ectopic muscle projection in the second pharyngeal arch, and the intermandibularis posterior muscles overextended in 58.3% of embryos (n = 64).

    Talarozole purchased from MCE. Usage Cited in: Mol Pharmacol. 2016 May;89(5):560-74.  [Abstract]

    Induction of hepatic mitochondrial biogenesis genes in mice after Talarozole (TLZ) treatment compared with vehicle-treated mice. All mRNA data are presented as fold change in mRNA abundance relative to control mice. β-Actin is used as the housekeeping gene. For protein data, results are expressed as ratio of SDHA to β-actin.

    查看 RAR/RXR 亚型特异性产品:

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    RXRα RXRβ RXRγ

    查看 Cytochrome P450 亚型特异性产品:

    查看所有亚型
    CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.

    IC50 & Target

    CYP26

     

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    Sf9 IC50
    0.00046 μM
    Compound: 3; R115866
    Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase
    Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase
    		[PMID: 26918322]
    Sf9 IC50
    0.0051 μM
    Compound: 3; R115866
    Inhibition of microsomal fraction of human CYP26A1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 1 min by HPLC analysis in presence of rat P450 reductase
    Inhibition of microsomal fraction of human CYP26A1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 1 min by HPLC analysis in presence of rat P450 reductase
    		[PMID: 26918322]
    体外研究
    (In Vitro)

    When HepG2 cells are cotreated with atRA and Talarozole (1 μM), 4-OH-RA and 4-oxo-RA formation is significantly decreased[2].

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

    Talarozole 相关抗体:
    体内研究
    (In Vivo)

    A maximum 84% inhibition of CYP26 activity at 0.5 hours post-dose is predicted based on Talarozole (TLZ) Cmax of 80 nM and a Ki of 1 nM following a single dose of Talarozole. Due to the short Talarozole half-life (2.2 hrs) CYP26 activity is predicted to return to 100% by 12 hours. In agreement with the predictions, atRA concentrations are increased by 82, 63 and 60% at 4 hours post-dose in the serum, liver and testes, respectively, and concentrations returned to baseline by 24 hours. Following multiple doses of Talarozole, liver CYP26 mRNA and activity are increased suggesting autoinduction of CYP26 due to increased atRA concentrations. In agreement, atRA concentrations are elevated in serum and liver at all timepoints measured. This increase in atRA concentrations is associated with increased mRNA of the mitochondrial biogenesis markers PGC-1β and NRF-1 in comparison to control mice[3].

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

    377.51

    Formula

    C21H23N5S
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    他拉罗唑
    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 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 33.33 mg/mL (88.29 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.6489 mL 13.2447 mL 26.4894 mL
    5 mM 0.5298 mL 2.6489 mL 5.2979 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 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

    动物实验：

    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 mg/mL (5.30 mM); 悬浊液

      此方案可获得 ≥ 2 mg/mL（饱和度未知）的均匀悬浊液，悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例，取 100 μL 20.0 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% Corn Oil

      Solubility: ≥ 2 mg/mL (5.30 mM); 澄清溶液

      此方案可获得 ≥ 2 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。

      以 1 mL 工作液为例，取 100 μL 20.0 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

    只
    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: 99.61%

    COA (201 KB) LCMS (121 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [2]

    Human liver microsomes (0.2 mg/mL) are incubated with 4-OH-atRA (500 nM) and NADPH, NADP+ or NAD+ (each at 2 mM) in 100 mM KPi buffer pH 7.4. In addition, 4-OH-atRA is incubated with human liver microsomes in the presence and absence of Talarozole (1 μM), a CYP26A1 specific inhibitor, and Ketoconazole (10 μM) a pan-P450 inhibitor and with NADPH as a cofactor. Following a 5 min pre-incubation, the reactions are initiated with the addition of cofactor and incubated for 30 minutes. At 30 min the reactions are quenched with equal volume of Acetonitrile and centrifuged at 3,000 g for 15 min. The supernatants are collected and 4-oxo-atRA formation is analyzed by LC-MS/MS. All incubations are normalized to a no cofactor control[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Mice[3]
    Talarozole is administered to mice as a single dose (2.5 mg/kg) or as multiple doses for three days. Serum Talarozole concentrations and serum, liver and testes atRA concentrations are measured by LC-MS/MS. Inhibition of CYP26 and changes inatRA concentrations in each tissue are predicted based on CYP26 activity in vitro and Talarozole disposition. Markers of fatty acid oxidation in the liver and spermatogonial differentiation in the testes are measured following Talarozole treatment.

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

    Talarozole 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6489 mL 13.2447 mL 26.4894 mL 66.2234 mL
    5 mM 0.5298 mL 2.6489 mL 5.2979 mL 13.2447 mL
    10 mM 0.2649 mL 1.3245 mL 2.6489 mL 6.6223 mL
    15 mM 0.1766 mL 0.8830 mL 1.7660 mL 4.4149 mL
    20 mM 0.1324 mL 0.6622 mL 1.3245 mL 3.3112 mL
    25 mM 0.1060 mL 0.5298 mL 1.0596 mL 2.6489 mL
    30 mM 0.0883 mL 0.4415 mL 0.8830 mL 2.2074 mL
    40 mM 0.0662 mL 0.3311 mL 0.6622 mL 1.6556 mL
    50 mM 0.0530 mL 0.2649 mL 0.5298 mL 1.3245 mL
    60 mM 0.0441 mL 0.2207 mL 0.4415 mL 1.1037 mL
    80 mM 0.0331 mL 0.1656 mL 0.3311 mL 0.8278 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.

    Keywords:

    Talarozole201410-53-9R115866他拉罗唑R 115866R-115866RAR/RXRCytochrome P450AutophagyRetinoic acid receptorsRetinoid X receptorsCYPsInhibitorinhibitorinhibit

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