BMS 961
(Synonyms: BMS 189961) 目录号 : GC17382A RAR? agonist
Cas No.:185629-22-5
Sample solution is provided at 25 µL, 10mM.
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BMS961 is a potent and selective retinoic acid receptor gamma (RARγ) agonist with IC50 values of 30 nM.
RARγ belongs to the family of nuclear receptors which regulates transcription. RARγ mediates the anti-proliferative and apoptotic effects of retinoids in cancer cells such as neuroblastoma cells. RARγ is the principal receptor that regulates RA mediated growth arrest in keratinocytes.
In vitro, application of BMS961on mouse ear skin was found to cause a significant increase of thymic stromal lymphopoietin (TSLP) transcripts1. In addition, exposure of BMS861 on limbs at low concentration leads to retarded growth of the zeugopod (long bones) and intactness of autopod (paw). However, high concentration of BMS961treatment caused equal undifferentiation of both limb regions 2.
In WT mice, RARγ agonists BMS961treatment resulted in an increase of the ear TSLP transcripts and serum TSLP, which indicates an involvement of RAR-mediated events in transcriptional activation of TSLP expression1.
References:
1. Li M, Hener P, Zhang Z, et al. Topical vitamin D3 and low-calcemic analogs induce thymic stromal lymphopoietin in mouse keratinocytes and trigger an atopic dermatitis. Proceedings of the National Academy of Sciences of the United States of America. 2006;103(31):11736-11741.
2. Galdones E, Hales BF. Retinoic acid receptor gamma-induced misregulation of chondrogenesis in the murine limb bud in vitro. Toxicological sciences : an official journal of the Society of Toxicology. 2008;106(1):223-232.
| Cas No. | 185629-22-5 | SDF | |
| 别名 | BMS 189961 | ||
| 化学名 | (S)-3-fluoro-4-(2-hydroxy-2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)acetamido)benzoic acid | ||
| Canonical SMILES | FC1=CC(C(O)=O)=CC=C1NC([C@H](C2=CC=C3C(C)(C)CCC(C)(C)C3=C2)O)=O | ||
| 分子式 | C23H26FNO4 | 分子量 | 399.46 |
| 溶解度 | <39.95mg/ml in DMSO | 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 | 2.5034 mL | 12.5169 mL | 25.0338 mL |
| 5 mM | 0.5007 mL | 2.5034 mL | 5.0068 mL |
| 10 mM | 0.2503 mL | 1.2517 mL | 2.5034 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