CD 3254
目录号 : GC17730
A selective RXR agonist
Cas No.:196961-43-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
CD3254 is a potent and selective agonist of Retinoid X receptors (RXRα).
Retinoid X receptors (RXRs) are nuclear receptors that act as ligand-dependent transcription factors and function as the homodimer or as heterodimers with other nuclear receptors, such as retinoic acid receptors (RARs), peroxisome proliferator-activated receptors (PPARs), or liver X receptors (LXRs). RXR plays essential roles in the regulation of glucose metabolism, lipid metabolism and immune response. Retinoid X receptors (RXRs) contains three family members including RARα, RARβ or RARγ receptors. RXRα belongs to the NR2B nuclear receptor family and primarily expressed in the liver, intestines, kidneys, and epidermis.
CD3254 and its’ analogue bexarotene have been reported as a treatment for cutaneous T-cell lymphoma (CTCL), despite the fact that treatment with CD3254 can evoke reactions by disturbing other RXR-heterodimer receptor pathways. Of the seven displayed novel exacerbates, all analogs animate RXR-controlled translation in mammalian 2 hybrid and RXRE-interceded tests, have equivalent or hoisted natural action in view of EC50 profiles, and hold comparative or enhanced apoptotic movement in CTCL assays contrasted with CD3254. Every single novel compound show selectivity for RXR and insignificant hybrid onto the retinoic corrosive receptor (RAR) contrasted with all-trans-retinoic corrosive, with select analogs likewise decreasing hindrance of other RXR-subordinate pathways (e.g., VDR-RXR) [1].
In vivo, CD3254 induced the phenotypes of malformations after 5 days exposure at low concentration (20 μg/l) to those after the 1st d exposure at high concentrations (50 and 100 μg/L) [2].
References:
Modeling, synthesis, and biological evaluation of potential retinoid X receptor (RXR) selective agonists: novel analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene) and (E)-3-(3-(1,2,3,4-tetrahydro-1,1,4,4,6-pentamethylnaphthalen-7-yl)-4-hydroxyphenyl)acrylic acid (CD3254). J Med Chem. 2013 Nov 14;56(21):8432-54. doi: 10.1021/jm4008517. Epub 2013 Nov 1.
Divergent teratogenicity of agonists of retinoid X receptors in embryos of zebrafish (Danio rerio). Ecotoxicology. 2012 Jul;21(5):1465-75. doi: 10.1007/s10646-012-0900-9. Epub 2012 Apr 10.
| Cas No. | 196961-43-0 | SDF | |
| 化学名 | (E)-3-(4-hydroxy-3-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)phenyl)acrylic acid | ||
| Canonical SMILES | OC1=CC=C(/C=C/C(O)=O)C=C1C2=C(C)C=C3C(C)(C)CCC(C)(C)C3=C2 | ||
| 分子式 | C24H28O3 | 分子量 | 364.48 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2)(1:8): 0.11 mg/ml,Ethanol: 20 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 | 2.7436 mL | 13.7182 mL | 27.4363 mL |
| 5 mM | 0.5487 mL | 2.7436 mL | 5.4873 mL |
| 10 mM | 0.2744 mL | 1.3718 mL | 2.7436 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。