Gigantol
(Synonyms: 大叶兰酚) 目录号 : GC33304
Gigantol是一种来自几种药用兰花的联苄基化合物。Gigantol对癌症有潜在治疗价值。Gigantol是Wnt/β-catenin通路的抑制剂。
Cas No.:67884-30-4
Sample solution is provided at 25 µL, 10mM.
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Gigantol is a bibenzyl compound derived from several medicinal orchids. Giganto shows promising therapeutic potential against cancer cells. Gigantol is a novel inhibitor of the Wnt/β-catenin pathway.
Gigantol decreases the level of phosphorylated LRP6 and cytosolic β-catenin in HEK293 cells. In breast cancer MDA-MB-231 and MDA-MB-468 cells, treatment with gigantol reduces the level of phosphorylated LRP6[1]. Gigantol significantly inhibits the proliferation and induces apoptosis of the HepG2 cells. Gigantol at concentrations of 1, 40 and 150 µM markedly decreases the cell viability by 11.7, 30.0 and 56.4% at 24 h and 21.1, 66.8 and 85.5% at 48 h, respectively. The IC50 value is 9.30 µM[2].
LDD and gigantol (25-100 mg/kg, p.o.) significantly increase the hot-plate latency in comparison to vehicle-treated mice and decreased carrageenaninduced inflammation in rats[2].
[1]. Yu S, et al. Gigantol inhibits Wnt/β-catenin signaling and exhibits anticancer activity in breast cancer cells. BMC Complement Altern Med. 2018 Feb 14;18(1):59. [2]. Chen H, et al. Gigantol attenuates the proliferation of human liver cancer HepG2 cells through the PI3K/Akt/NF-κB signaling pathway. Oncol Rep. 2017 Feb;37(2):865-870. [3]. Déciga-Campos M, et al. Antinociceptive and anti-inflammatory effects of compounds isolated from Scaphyglottis livida and Maxillaria densa. J Ethnopharmacol. 2007 Nov 1;114(2):161-8.
Cell experiment: | HepG2 cells are treated with a series of concentrations of Gigantol (1, 10, 40, 80 and 150 µM) for different time intervals (12, 24 and 48 h). The cytotoxicity is measured using MTT assays[2]. |
Animal experiment: | Rats[3]The anti-inflammatory activity is determined by carrageenan-induced edema test in the hind paws of rats. Sprague-Dawley rats are fasted for 15 h before the experiment with free access to water. One hundred microlitres of 1% carrageenan (10 mg/mL, Type IV, lambda) suspension is prepared 30 min before each experiment and injected into the plantar side of right hindpaw of the rats. The CH2Cl2-MeOH Scaphyglottis livida and Maxillaria densa extracts (150-600 mg/kg), as well as compound LDD and gigantol (25-100 mg/kg), are orally administered. The extracts, LDD and gigantol are administered 1 h before the carrageenan treatment[3].Mice[3]Mice receive an oral administration of vehicle (0.2% Tween-80) or increasing doses of Scaphyglottis livida and Maxillaria densa extracts (150–600 mg/kg) or LDD and gigantol (25-100 mg/kg) 30 min before the thermal noxious stimuli in the hot-plate test. Morphine (1.5-6 mg/kg, p.o.) is used as positive control. Mice are observed before and at 30, 60, 90 and 120 min after drugs administration[3]. |
References: [1]. Yu S, et al. Gigantol inhibits Wnt/β-catenin signaling and exhibits anticancer activity in breast cancer cells. BMC Complement Altern Med. 2018 Feb 14;18(1):59. | |
| Cas No. | 67884-30-4 | SDF | |
| 别名 | 大叶兰酚 | ||
| Canonical SMILES | COC1=CC(O)=CC(CCC2=CC(O)=C(OC)C=C2)=C1 | ||
| 分子式 | C16H18O4 | 分子量 | 274.31 |
| 溶解度 | DMSO : ≥ 160 mg/mL (583.28 mM) | 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 | 3.6455 mL | 18.2276 mL | 36.4551 mL |
| 5 mM | 0.7291 mL | 3.6455 mL | 7.291 mL |
| 10 mM | 0.3646 mL | 1.8228 mL | 3.6455 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet