DY131
(Synonyms: GSK 9089;DY-131;DY 131;GSK9089;GSK-9089) 目录号 : GC10394
An ERRβ/γ agonist
Cas No.:95167-41-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: N/A
DY131 is an agonist ligand for estrogen-related receptors ERRβ/γ. Estrogen receptor-related receptors (ERR) are orphan nuclear receptors constitutively activated without estrogen binding. ERRs may be involved in similar ER-mediated regulatory pathways and modulate estrogen responsiveness in certain target cells. The ERR subtypes, ERRβ/γ, are coexpressed in normal human prostatic epithelial cells and exhibit reduced expression in many prostate cancer cell lines.
In vitro: DY131 was evaluated for its selectivity and efficacy in modulating the transcriptional activity of ERRα/β/γ and ERβ/γ. CV-1 cells were transfected with reporter constructs or expression vectors and the fold activation of the reporter construct was determined at different concentrations of DY131. DY131 was found to be not able to activate the reporter construct or ERRα at any of the tested concentrations. In contrast, DY131 led to three- to fourfold activation of ERRβ at concentrations of 10-30 μM. Activity on ERRγ was more pronounced with five-fold activation at 3 μM and maximal 6.6-fold activity observed at 30 μM. Thus, DY131 was an selective ERRβ/γ ligand displaying preferential selectivity for ERRγ at lower concentrations [1].
In vivo: Currently, there is no animal in vivo data available for DY131 and its analogs.
Clinical trial: So far, no clinical study has been reported for DY131 and its analogs.
Reference:
[1] Yu DD,Forman BM. Identification of an agonist ligand for estrogen-related receptors ERRbeta/gamma. Bioorg Med Chem Lett.2005 Mar 1;15(5):1311-3.
| Cas No. | 95167-41-2 | SDF | |
| 别名 | GSK 9089;DY-131;DY 131;GSK9089;GSK-9089 | ||
| 化学名 | N-[(E)-[4-(diethylamino)phenyl]methylideneamino]-4-hydroxybenzamide | ||
| Canonical SMILES | CCN(CC)C1=CC=C(C=C1)C=NNC(=O)C2=CC=C(C=C2)O | ||
| 分子式 | C18H21N3O2 | 分子量 | 311.38 |
| 溶解度 | ≥ 37.1 mg/mL in DMSO, ≥ 6.91 mg/mL in EtOH with ultrasonic and warming | 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 | 3.2115 mL | 16.0576 mL | 32.1151 mL |
| 5 mM | 0.6423 mL | 3.2115 mL | 6.423 mL |
| 10 mM | 0.3212 mL | 1.6058 mL | 3.2115 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。