Arbutin-d4(Synonyms: β-Arbutin-d4)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Arbutin-d4 (Synonyms: β-Arbutin-d4)

Arbutin-d4 是 Arbutin 氘代物。Arbutin (β-Arbutin) 是一种从熊果植物 Arctostaphylos uvaursi 中分离出的天然多酚,具有抗氧化,抗炎和抗肿瘤特性。是黑色素细胞中酪氨酸酶 (tyrosinase) 的竞争性抑制剂,对单酚酶的 Kiapp 值为 1.42 mM;对二酚酶 Kiapp 的值为 0.9 mM。Arbutin 也用作脱色剂。

Arbutin-d4(Synonyms: β-Arbutin-d4)

Arbutin-d4 Chemical Structure

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生物活性

Arbutin-d4 is deuterium labeled Arbutin. Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase in melanocytes, with Kiapp values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents[1]. Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties[2][3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

276.28

Formula

C12H12D4O7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Garcia-Jimenez A, et al. Action of tyrosinase on alpha and beta-arbutin: A kinetic study. PLoS One. 2017 May 11;12(5):e0177330.

    [3]. Jiang L, et al. Investigation of the pro-apoptotic effects of arbutin and its acetylated derivative on murinemelanoma cells. Int J Mol Med. 2018 Feb;41(2):1048-1054.

    [4]. Nalban N, et al. Arbutin Attenuates Isoproterenol-Induced Cardiac Hypertrophy by Inhibiting TLR-4/NF-κB Pathway in Mice. Cardiovasc Toxicol. 2019 Sep 4.

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Arbutin(Synonyms: 熊果苷; β-Arbutin)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Arbutin (Synonyms: 熊果苷; β-Arbutin) 纯度: ≥98.0%

Arbutin (β-Arbutin) 是一种从熊果植物 Arctostaphylos uvaursi 中分离出的天然多酚,具有抗氧化,抗炎和抗肿瘤特性。是黑色素细胞中酪氨酸酶 (tyrosinase) 的竞争性抑制剂,对单酚酶的 Kiapp 值为 1.42 mM;对二酚酶 Kiapp 的值为 0.9 mM。Arbutin 也用作脱色剂。

Arbutin(Synonyms: 熊果苷; β-Arbutin)

Arbutin Chemical Structure

CAS No. : 497-76-7

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10 g ¥910 In-stock
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Arbutin 相关产品

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生物活性

Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase in melanocytes, with Kiapp values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents[1]. Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties[2][3].

IC50 & Target

Tyrosinase[1]

体外研究
(In Vitro)

Arbutin (0.3-5.4 mM; 24 hours, 48 hours, 72 hours; B16 murine melanoma cells) inhibites the viability of B16 murine melanoma cells in a time-and dose-dependent manner[2].
Arbutin (1.4-5.4 mM; 24 hours) increases the apoptosis rate of B16 murine melanoma cell of treatment at a dose of 5.4 mM[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: B16 murine melanoma cells
Concentration: 0.3 mM, 0.7 mM, 1.4 mM, 2.1 mM, 2.9 mM, 3.6 mM, 5.4 mM
Incubation Time: 24 hours, 48 hours or 72 hours
Result: Inhibited the viability of B16 murine melanoma cells in a time- and dose-dependent manner.

Apoptosis Analysis[2]

Cell Line: B16 murine melanoma cells
Concentration: 1.4 mM, 2.9 mM, 5.4 mM
Incubation Time: 24 hours
Result: Caused apoptosis in 19.3% of the cells.

体内研究
(In Vivo)

Arbutin (50 mg/kg, 100 mg/kg; oral administration; every day; for 17 days; male C57BL/6 mice) pretreatment exhibits markedly protective effects on ISO-induced cardiac hypertrophy in mice[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 mice ( 20-25 g)[3]
Dosage: 50 mg/kg, 100 mg/kg
Administration: Oral administration; every day; for 17 days
Result: Ameliorated the ISO-induced myocardial injury.

分子量

272.25

Formula

C12H16O7

CAS 号

497-76-7

中文名称

熊果苷;熊果酚甙;熊果素;熊果叶甙;楊梅葉甘

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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (183.65 mM)

H2O : 33.33 mg/mL (122.42 mM; Need ultrasonic)

* “≥” 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 3.6731 mL 18.3655 mL 36.7309 mL
5 mM 0.7346 mL 3.6731 mL 7.3462 mL
10 mM 0.3673 mL 1.8365 mL 3.6731 mL

*

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。-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。

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

  • 1.

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

    Solubility: ≥ 2.5 mg/mL (9.18 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.18 mM,饱和度未知) 的澄清溶液。

    以 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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (9.18 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.18 mM,饱和度未知) 的澄清溶液。

    以 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.18 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.18 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Garcia-Jimenez A, et al. Action of tyrosinase on alpha and beta-arbutin: A kinetic study. PLoS One. 2017 May 11;12(5):e0177330.

    [2]. Jiang L, et al. Investigation of the pro-apoptotic effects of arbutin and its acetylated derivative on murinemelanoma cells. Int J Mol Med. 2018 Feb;41(2):1048-1054.

    [3]. Nalban N, et al. Arbutin Attenuates Isoproterenol-Induced Cardiac Hypertrophy by Inhibiting TLR-4/NF-κB Pathway in Mice. Cardiovasc Toxicol. 2019 Sep 4.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务