BMS 493
(Synonyms: BMS 204493) 目录号 : GC15648
A pan-RAR inverse agonist
Cas No.:215030-90-3
Sample solution is provided at 25 µL, 10mM.
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BMS493 is an inverse agonist of pan-retinoic acid receptors (pan-RARs). This compound has been shown to increase nuclear corepressor (NCoR) interaction with RARs.
The retinoic acid receptor (RAR), a type of nuclear receptor , is a ligand-dependent transcription factor that is activated by 9-cis retinoic acid and all-trans retinoic acid. Binding of agonist ligands to RAR results in dissociation of corepressor and recruitment of coactivator protein that, in turn, promotes transcription of the downstream target gene into mRNA and eventually protein. This protein controls a number of physiological processes including cell growth, differentiation, survival, and death.
In cellular culture, pretreatment of BMS493 on MEPM cells blocked atRA-induced apoptotic indexes. Mechanistically, this component completely inhibited atRA-induced Sub-G1 fraction, DNA fragmentation, and caspase-3 activation.1.
In vivo, inhibition of RAR signaling with BMS493 induced a very high degree of congenital diaphragmatic hernia, which was associated with a marked left–right sidedness that depended on the timing of drug delivery2.
References:
1. Yu Z, Han J, Lin J, et al. Apoptosis induced by atRA in MEPM cells is mediated through activation of caspase and RAR. Toxicological sciences : an official journal of the Society of Toxicology. 2006;89(2):504-509.
2. Clugston RD, Zhang W, Alvarez S, et al. Understanding abnormal retinoid signaling as a causative mechanism in congenital diaphragmatic hernia. American journal of respiratory cell and molecular biology. 2010;42(3):276-285.
| Cas No. | 215030-90-3 | SDF | |
| 别名 | BMS 204493 | ||
| 化学名 | (E)-4-(2-(5,5-dimethyl-8-(phenylethynyl)-5,6-dihydronaphthalen-2-yl)vinyl)benzoic acid | ||
| Canonical SMILES | OC(C1=CC=C(C=C1)/C=C/C2=CC=C3C(C)(C)CC=C(C#CC4=CC=CC=C4)C3=C2)=O | ||
| 分子式 | C29H24O2 | 分子量 | 404.5 |
| 溶解度 | 25mg/mL in DMSO, 30mg/mL in DMF | 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 | 2.4722 mL | 12.3609 mL | 24.7219 mL |
| 5 mM | 0.4944 mL | 2.4722 mL | 4.9444 mL |
| 10 mM | 0.2472 mL | 1.2361 mL | 2.4722 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet