Dihydrotanshinone I
(Synonyms: 二氢丹参酮 I) 目录号 : GN10617
A diterpene tanshinone with diverse biological activities
Cas No.:87205-99-0
Sample solution is provided at 25 µL, 10mM.
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Dihydrotanshinone I is a natural compound extracted from Salvia miltiorrhiza Bunge which has been widely used for treating cardiovascular diseases.
In lipopolysaccharide (LPS)-stimulated human umbilical vein endothelial cells (HUVECs), DHT (10 nM) decreases lectin-like ox-LDL receptor-1 (LOX-1) and NADPH oxidase 4 (NOX4) expression, reactive oxygen species (ROS) production, NF-κB nuclear translocation, ox-LDL endocytosis and monocytes adhesion[1]. Dihydrotanshinone I induces caspase dependent apoptosis induced in HCT116 cells. Dihydrotanshinone I induces concentration and ROS dependent caspase activation. Apoptosis induced by Dihydrotanshinone I is completely prevented by Z-VAD-fmk. Apoptosis induced by Dihydrotanshinone I is significantly inhibited by pretreatment of Z-LEHD-fmk but only is partially inhibited by Z-IETD-fmk. Apoptosis induced by Dihydrotanshinone I is significantly increased by caspase-2 knockdown[3].
DHT (10 and 25 mg/kg) significantly attenuates atherosclerotic plaque formation, alteres serum lipid profile, decreases oxidative stress and shrinks necrotic core areas in ApoE-/- mice. DHT dramatically inhibits the enhanced expression of LOX-1, NOX4, and NF-κB in aorta[1]. Dihydrotanshinone I (1, 2, 4 mg/kg) treatment can improve cardiac function, reduce infarct size, ameliorate the variations in myocardial zymogram and histopathological disorders, decrease 20-HETE generation, and regulate apoptosis-related protein in myocardial ischemia-reperfusion rats[2].
References:
[1]. Zhao W, et al. Dihydrotanshinone I Attenuates Atherosclerosis in ApoE-Deficient Mice: Role of NOX4/NF-κB Mediated Lectin-Like Oxidized LDL Receptor-1 (LOX-1) of the Endothelium. Front Pharmacol. 2016 Nov 8;7:418. eCollection 2016.
[2]. Wei Y, et al. The cardioprotection of dihydrotanshinone I against myocardial ischemia-reperfusion injury via inhibition of arachidonic acid ω-hydroxylase. Can J Physiol Pharmacol. 2016 Dec;94(12):1267-1275. Epub 2016 Jun 24.
[3]. Wang L, et al. Dihydrotanshinone I induced apoptosis and autophagy through caspase dependent pathway in colon cancer. Phytomedicine. 2015 Nov 15;22(12):1079-87.
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Kinase experiment: |
Cells are treated with various concentrations of Dihydrotanshinone I (3.13-20 µM) for 48 h. For the activity assay, Ac-DEVD-AMC (1 µg/µL), Ac-IETD-AMC (1 µg/µL) or Ac-LEDH-AMC (1 µg/µL) and cell lysate are added into Protease Assay Buffer in 96-well plate. Reaction mixtures with lysis buffer are used as negative controls. Cells treated with DMSO (0.1%) are treated as vehicle control. The reaction mixtures are incubated for 1 h at 37°C. The AMC liberated from the substrates is measured using spectrofluorometer of Victor 2 plate reader with an excitation wavelength of 380 nm and an emission wavelength of 430 nm. |
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Animal experiment: |
Male ApoE-/- mice (6-8 weeks old) on C57BL/6J background and age-matched wild-type C57BL/6J controls housed in SPF-grade animal facilities with a 12 h light/dark cycle, at 23°C (±2°C). Starting from 6 weeks, the mice are fed with a HCD (54.35% raw grain, 20% lard, 0.15% cholesterol, 15% sucrose, 0.5% Sodium Cholate, 10% yolk powder) for 12 weeks. All ApoE-/- mice are dosed daily via intragastric gavage with 10 and 25 mg/kg Dihydrotanshinone I dissolved in 0.5% CMC-Na or administered 0.5% CMC-Na alone (vehicle control) (n=8 per group). |
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References: [1]. Zhao W, et al. Dihydrotanshinone I Attenuates Atherosclerosis in ApoE-Deficient Mice: Role of NOX4/NF-κB Mediated Lectin-Like Oxidized LDL Receptor-1 (LOX-1) of the Endothelium. Front Pharmacol. 2016 Nov 8;7:418. eCollection 2016. |
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| Cas No. | 87205-99-0 | SDF | |
| 别名 | 二氢丹参酮 I | ||
| 化学名 | (1R)-1,6-dimethyl-1,2-dihydronaphtho[1,2-g][1]benzofuran-10,11-dione | ||
| Canonical SMILES | CC1COC2=C1C(=O)C(=O)C3=C2C=CC4=C3C=CC=C4C | ||
| 分子式 | C18H14O3 | 分子量 | 278.3 |
| 溶解度 | DMF: 0.2 mg/ml,DMSO: 0.2 mg/ml | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5932 mL | 17.9662 mL | 35.9324 mL |
| 5 mM | 0.7186 mL | 3.5932 mL | 7.1865 mL |
| 10 mM | 0.3593 mL | 1.7966 mL | 3.5932 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet