DWK-1339 (MDR-1339)
(Synonyms: DWK-1339) 目录号 : GC31083
An inhibitor of amyloid-β aggregation
Cas No.:1018946-38-7
Sample solution is provided at 25 µL, 10mM.
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DWK-1339 is an inhibitor of amyloid-β (Aβ) aggregation.1 It inhibits aggregation of monomeric Aβ (1-42) (Aβ42) and induces disaggregation of Aβ42 fibrils in vitro when used at concentrations ranging from 3.1 to 50 ?M. DWK-1339 (10 ?M) reduces Aβ42-induced toxicity in HT-22 cells. In vivo, DWK-1339 (10 mg/kg) increases step-through latency in a passive avoidance test and increases spontaneous alteration in the Y-maze compared with vehicle control mice in a mouse model of Aβ42-induced acute Alzheimer's disease. It also decreases brain levels of Aβ42 and increases spontaneous alteration in the Y-maze in the APP/PS1 transgenic mouse model of Alzheimer's disease.
1.Ha, H., Kang, D.W., Kim, H.-M., et al.Discovery of an orally bioavailable benzofuran analogue that serves as a β-amyloid aggregation inhibitor for the potential treatment of Alzheimer's diseaseJ. Med. Chem.61(1)396-402(2018)
Cell experiment: | HT22 cells, a murine cell line of hippocampal origin, are grown in Dulbecco's modified Eagle's medium (DMEM) containing 10% fetal bovine serum and 5% penicillin/streptomycin. At the outset, 90% confluent cells are dissociated and plated at 5 × 103 cells/well in a 96-well plate. When the cells are attached to the plate, the medium is replaced with plain DMEM. The cells are treated with MDR-1339. One hour after MDR-1339 treatment, 4 μL of pre-diluted 25 μM Aβ42 is added to the media, and the cells are further incubated for 18 h. For the determination of cell viability, 15 μL of 5 mg/mL MTT is added to each well and incubated for 3 h. The formazan that formed is dissolved in DMSO, and the absorbance is measured at 570-630 nm using a plate reader[1]. |
Animal experiment: | For this study, a total of 24 (n = 8 for each group) APP/PS1 [B6C3-Tg (APPswe, PSEN1dE9) 85Dbo/J] Tg mice are utilized. The mice are housed in a controlled environment under standard room temperature, relative humidity and a 12 h light/dark cycle with free access to food and water. APP/PS1 treated groups are orally administered with MDR-1339 at a dose of 30 or 100 mg/kg body weight once daily. MDR-1339 treatment is at the age of 29 weeks, and the treatment is conducted for 8 weeks[1]. |
References: [1]. Ha HJ, et al. Discovery of an Orally Bioavailable Benzofuran Analogue That Serves as a β-Amyloid Aggregation Inhibitor for the Potential Treatment of Alzheimer's Disease. J Med Chem. 2018 Jan 11;61(1):396-402. | |
| Cas No. | 1018946-38-7 | SDF | |
| 别名 | DWK-1339 | ||
| Canonical SMILES | COCCCC1=CC=C(OC(C2=CC=C(OC)C(OC)=C2)=C3)C3=C1 | ||
| 分子式 | C20H22O4 | 分子量 | 326.39 |
| 溶解度 | DMSO : ≥ 83.3 mg/mL (255.22 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 | 3.0638 mL | 15.3191 mL | 30.6382 mL |
| 5 mM | 0.6128 mL | 3.0638 mL | 6.1276 mL |
| 10 mM | 0.3064 mL | 1.5319 mL | 3.0638 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet