CD 2665
目录号 : GC12072A selective RARβ and RARγ antagonist
Cas No.:170355-78-9
Sample solution is provided at 25 µL, 10mM.
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CD 2665 is a retinoic acid receptor β (RARβ) / RARγ antagonist [1] [2] [3] with binding Kd values of 306 nM and 110 nM to RARβ and RARγ, respectively [3].
Retinoic acid receptors include RARα, RARβ and RARγ. They are able to bind 9-cis and all-trans stereoisomers of retinoic acid (RA) [1], and mediate RA signal as transcription factors [2].
CD 2665 (1 µM) did not antagonize the luciferase activity induced by 9-cis- or all-trans-RA in HiB5 cells, but partially blocked the luciferase activity in 3XbRARE-Luc-transfected cells induced by CD 666 (a RARγ-selective agonist, 100 nM). CD 2665 at 1 µM reduced the viable cell number to about 60% level of vehicle-treated cells. CD 2665 (1 µM) clearly antagonized the increase in cell number resulted from the treatment with CD 666 (100 nM) [4].
The biosynthesis of retinoic acid can also be disordered by chronic ethanol consumption. CD 2665 administration did not modify blood alcohol levels in alcohol-treated mice, but totally reversed the impairment of spontaneous alternation rates resulted from alcohol consumption. Administration with CD2665 for 22 days in alcohol-treated mice significantly decreased both mRNA expression and enzymatic activity of tTG (a retinoic acid-target gene) and normalized the expression levels to the level in control mice [2].
References:
[1]. Yasmin Marikar, ZengQuan Wang, Elizabeth A. Duell, et al. Retinoic Acid Receptors Regulate Expression of Retinoic Acid 4-Hydroxylase that Specifically Inactivates All-Trans Retinoic Acid in Human Keratinocyte HaCaT Cells. The Journal of Investigative Dermatology, 1998, 111(3):434-439.
[2]. Serge Alfos, Catherine Boucheron, Véronique Pallet, et al. A Retinoic Acid Receptor Antagonist Suppresses Brain Retinoic Acid Receptor Overexpression and Reverses a Working Memory Deficit Induced by Chronic Ethanol Consumption in Mice. Alcohol Clin Exp Res., 2001, 25(10): 1506-1514.
[3]. Zsuzsa Szondy, Uwe Reichert, Jean-Michel Bernardon, et al. Inhibition of activation-induced apoptosis of thymocytes by all-trans- and 9-cis-retinoic acid is mediated via retinoic acid receptor α. Biochem. J., 1998, 331:767-774.
[4]. Jean-Ju Chung, Sehyung Cho, Yunhee Kim Kwon, et al. Activation of retinoic acid receptor γ induces proliferation of immortalized hippocampal progenitor cells. Molecular Brain Research, 2000, 83:52-62.
| Cas No. | 170355-78-9 | SDF | |
| 化学名 | 4-(7-((1s,3R,5S,7s)-adamantan-1-yl)-6-((2-methoxyethoxy)methoxy)naphthalen-2-yl)benzoic acid | ||
| Canonical SMILES | OC(C1=CC=C(C=C1)C2=CC=C3C(C=C(C(OCOCCOC)=C3)[C@]4(C[C@H](C5)C6)C[C@@H]5C[C@H]6C4)=C2)=O | ||
| 分子式 | C31H34O5 | 分子量 | 486.6 |
| 溶解度 | DMF: 30 mg/mL,DMF:PBS(pH 7.2)(1:1): 0.5 mg/mL,DMSO: 25 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 | 2.0551 mL | 10.2754 mL | 20.5508 mL |
| 5 mM | 0.411 mL | 2.0551 mL | 4.1102 mL |
| 10 mM | 0.2055 mL | 1.0275 mL | 2.0551 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