RS-246204
目录号 : GC33079
RS-246204是一种R-spondin-1替代化合物，能够在不使用R-spondin-1蛋白的情况下启动肠的类器官。
Cas No.:878451-87-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Mice[1]Seven-week-old C57Bl/6 mice are given a 2.5% dextran sulfate sodium treatment in drinking water for 5 days. RS-246204 (10 mg/kg in DMSO) is administered intraperitoneally at the end of the DSS exposure. The RS-246204 treatment is repeated every 24 h for 5 days. Daily assessments of disease activity are performed including measuring body weight and evaluating stool consistency. The mice are sacrificed the next day after the last injection of RS-246204. BrdU (50 mg/kg in saline) is administered intraperitoneally 24 hours before sacrifice[1]. |
References: [1]. Nam MO, et al. Effects of a small molecule R-spondin-1 substitute RS-246204 on a mouse intestinal organoid culture. Oncotarget. 2017 Dec 26;9(5):6356-6368. | |
RS-246204 is a R-spondin-1 substitute compound that is able initiate small intestinal organoids without the use of the R-spondin-1 protein.
R-spondin-1 protein is added at a high concentration for the initiation and maintenance of the organoids. RS-246204 is a R-spondin-1 substitute that could promote the initial formation and growth of enteroids in the medium without R-spondin-1. The enteroids grown with RS-246204 had a similar differentiation capacity as well as self-renewal capacity as the enteroids grown with R-spondin-1. Furthermore, the RS-246204-derived enteroids could successfully produce the forskolin induced swelling and the organoid based epithelial to mesenchymal transition model[1].
RS-246204 significantly increased BrdU+ cells and body weight in the DSS induced colitis model. These results suggest that RS-246204 activates the R-spondin dependent pathway in Lgr5 stem cells, thereby enhancing proliferation or the anti-apoptotic effect, promoting regeneration of the intestinal epithelium and reducing the disease severity[1].
[1]. Nam MO, et al. Effects of a small molecule R-spondin-1 substitute RS-246204 on a mouse intestinal organoid culture. Oncotarget. 2017 Dec 26;9(5):6356-6368.
| Cas No. | 878451-87-7 | SDF | |
| Canonical SMILES | O=C(N1)N(C)C2=C(N(C)C(SC3=NC4=CC=CC=C4C=C3)=N2)C1=O | ||
| 分子式 | C16H13N5O2S | 分子量 | 339.37 |
| 溶解度 | DMSO : 5 mg/mL (14.73 mM);Water : < 0.1 mg/mL (insoluble) | 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 | 2.9466 mL | 14.7332 mL | 29.4664 mL |
| 5 mM | 0.5893 mL | 2.9466 mL | 5.8933 mL |
| 10 mM | 0.2947 mL | 1.4733 mL | 2.9466 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。
Effects of a small molecule R-spondin-1 substitute RS-246204 on a mouse intestinal organoid culture
Oncotarget 2017 Dec 26;9(5):6356-6368.PMID:29464078DOI:PMC5814218
Organoids, a multi-cellular and organ-like structure cultured in vitro, can be used in a variety of fields such as disease modeling, drug discovery, or cell therapy development. When organoids derived from Lgr5 stem cells are cultured ex vivo, recombinant R-spondin-1 protein should be added at a high concentration for the initiation and maintenance of the organoids. Because the addition of large amounts of R-spondin-1 greatly increases the cost of organoids, the organoids grown with R-spondin-1 are not practical for large-scale drug screening and for the development of therapeutic agents. In this study, we tried to find a R-spondin-1 substitute compound that is able initiate small intestinal organoids without the use of the R-spondin-1 protein; thus, using organoid media that each included one compound from among an 8,364 compound library instead of R-spondin-1, we observed whether organoids were established from the crypts of the small intestine. As a result, we found one compound that could promote the initial formation and growth of enteroids in the medium without R-spondin-1 and named it RS-246204. The enteroids grown with RS-246204 had a similar differentiation capacity as well as self-renewal capacity as the enteroids grown with R-spondin-1. Furthermore, the RS-246204-derived enteroids could successfully produce the forskolin induced swelling and the organoid based epithelial to mesenchymal transition model. This compound could be used for developing a cost-efficient culturing method for intestinal organoids as well as for exploring Lgr5 signaling, intestinal stem cell physiology and therapeutics for GI tract diseases.