| Size | Price | Stock | Qty |
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| Targets |
RS-246204 targets the R-spondin signaling pathway. It acts as a substitute for R-spondin-1, a protein that activates Wnt/β-catenin signaling by binding to LGR4/5/6 receptors and inhibiting the E3 ubiquitin ligases RNF43 and ZNRF3. By mimicking R-spondin-1, RS-246204 activates R-spondin-dependent pathways, promoting cell proliferation and tissue regeneration.
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| ln Vitro |
R-spondin-1 protein is introduced in high doses to begin and maintain organoids. In media lacking R-spondin-1, RS-246204, an R-spondin-1 substitute, stimulates the early development and proliferation of enteroids. Similar differentiation and self-renewal capacities are exhibited by intestinal cultures grown with RS-246204 and R-spondin-1. Moreover, organoid-based epithelial-mesenchymal transition models and forskolin-induced swelling can be effectively produced by enteroids derived from RS-246204 [1].
RS-246204 is a small molecule that substitutes for R-spondin-1 in vitro. It enables the initiation and maintenance of small intestinal organoids without the need for exogenous R-spondin-1 protein. This demonstrates its potent activity in stem cell culture and organoid models. |
| ln Vivo |
RS-246204 markedly elevated body weight and BrdU+ cells in the colitis model generated by DSS. These findings suggest that RS-246204 stimulates the R-spondin-dependent pathway in Lgr5 stem cells, which in turn promotes intestinal epithelial regeneration, lessens the severity of illness, and enhances proliferation or anti-apoptotic actions [1].
RS-246204 has demonstrated in vivo activity in the DSS-induced colitis model. It activates R-spondin-dependent pathways and promotes regeneration of injured intestinal epithelium. This confirms its ability to stimulate tissue regeneration in vivo and suggests potential therapeutic applications in inflammatory bowel disease and other intestinal disorders. |
| Enzyme Assay |
The in vitro activity of RS-246204 is assessed using organoid culture assays. Small intestinal stem cells are cultured in the presence of RS-246204 instead of R-spondin-1. The ability of the compound to support the initiation and maintenance of organoids is assessed by measuring organoid formation, growth, and viability.
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| Cell Assay |
Cell-based assays are used to evaluate RS-246204's ability to activate R-spondin-dependent signaling. Cells expressing LGR4/5/6 receptors are treated with RS-246204, and the activation of Wnt/β-catenin signaling is measured using reporter gene assays or by assessing the expression of Wnt target genes. The compound's ability to inhibit RNF43/ZNRF3-mediated ubiquitination can also be assessed.
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| Animal Protocol |
RS-246204 has been evaluated in the DSS-induced colitis model in mice. In these studies, the compound is typically administered to mice with DSS-induced intestinal injury, and its effects on intestinal epithelial regeneration, inflammation, and disease severity are assessed.
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| ADME/Pharmacokinetics |
RS-246204 has a molecular weight of 339.37 and a molecular formula of C16H13N5O2S. The IUPAC name is 3,7-Dimethyl-8-(quinolin-2-ylthio)-3,7-dihydro-1H-purine-2,6-dione. It is soluble in DMSO. Purity is typically 98% by HPLC. Powder should be stored at -20°C for up to 3 years.
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| Toxicity/Toxicokinetics |
RS-246204 is a research compound and its full toxicological profile is not detailed in the available literature. In the DSS-induced colitis model, it has been used to promote intestinal epithelial regeneration without significant adverse effects reported. Standard safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
RS-246204 (CAS#: 878451-87-7) is a small-molecule R-spondin-1 substitute that enables initiation and maintenance of small intestinal organoids without exogenous R-spondin-1. It activates R-spondin-dependent pathways and promotes regeneration of injured intestinal epithelium in DSS-induced colitis models. RS-246204 is a valuable research tool for studying stem cell biology, intestinal regeneration, and inflammatory bowel disease.
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| Molecular Formula |
C16H13N5O2S
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| Molecular Weight |
339.37
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| Exact Mass |
339.079
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| CAS # |
878451-87-7
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| PubChem CID |
6485821
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| Appearance |
White to light yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.784
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| LogP |
2.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
24
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| Complexity |
533
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1C2=C(N=C1SC3=NC4=CC=CC=C4C=C3)N(C(=O)NC2=O)C
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| InChi Key |
UHUHSGFUUWVRBO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H13N5O2S/c1-20-12-13(21(2)15(23)19-14(12)22)18-16(20)24-11-8-7-9-5-3-4-6-10(9)17-11/h3-8H,1-2H3,(H,19,22,23)
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| Chemical Name |
3,7-dimethyl-8-quinolin-2-ylsulfanylpurine-2,6-dione
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| Synonyms |
RS246204; RS 246204; RS-246204
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~5 mg/mL (~14.73 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 0.5 mg/mL (1.47 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (1.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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