| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
CYM-50260 targets the sphingosine-1-phosphate receptor 4 (S1P4), a G-protein-coupled receptor (GPCR) that mediates the effects of the bioactive lipid sphingosine-1-phosphate (S1P). It acts as a potent agonist with an EC50 of 45 nM. The compound is highly selective for S1P4, showing no activity at S1P1, S1P2, S1P3, or S1P5 at concentrations up to 25 µM.
|
|---|---|
| ln Vitro |
Synthetic S1P4-R agonist CYM50260 (Compound 22aa) is one of them. The hit compound (HTS-hit) is 3.5 times less powerful than CYM50260 [1]. PDGF-AB secretion, sCD40L release, and collagen-stimulated platelet aggregation are all inhibited by CYM50260. HSP27's phosphorylation and release of collagen-phosphorylated HSP27 are both decreased by CYM50260 [2].
In vitro, CYM-50260 acts as a potent and selective agonist of S1P4. It inhibits collagen-induced platelet aggregation, sCD40L release, and PDGF-AB secretion. These effects are consistent with the known roles of S1P4 in platelet function and immune regulation. The compound's high selectivity makes it a valuable tool for dissecting S1P4-specific signaling pathways. |
| ln Vivo |
No specific in vivo activity data is publicly available for CYM-50260. As a research compound, its in vivo efficacy and pharmacokinetic properties have not been extensively reported. Further studies would be needed to establish its in vivo activity, particularly in immune and inflammatory models where S1P4 signaling is being investigated.
|
| Enzyme Assay |
In cell-free receptor binding assays, CYM-50260's activity is evaluated by measuring its affinity and potency at the S1P4 receptor. Membrane preparations from cells expressing the human S1P4 receptor are incubated with a radiolabeled ligand (e.g., [33P]S1P) or a fluorescent tracer, and varying concentrations of the compound. The displacement of the tracer or the activation of downstream signaling (e.g., GTPγS binding) is measured to determine the Ki and EC50.
|
| Cell Assay |
In vitro cell-based experiments with CYM-50260 typically involve cell lines expressing the S1P4 receptor, such as CHO or HEK293 cells. Cells are treated with the compound, and receptor activation is assessed by measuring downstream signaling events, such as inhibition of forskolin-stimulated cAMP accumulation, calcium mobilization, or activation of MAP kinase pathways. The EC50 for receptor activation is determined from the concentration-response curve.
|
| Animal Protocol |
No specific in vivo animal protocols are publicly available for CYM-50260. If in vivo studies were to be conducted, typical protocols might involve mouse models of inflammation, thrombosis, or immune regulation, where the compound would be administered intraperitoneally or subcutaneously, and relevant endpoints (e.g., platelet aggregation, cytokine levels) would be measured.
|
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is publicly available for CYM-50260. As a research compound, its absorption, distribution, metabolism, and excretion (ADME) properties have not been extensively characterized. The compound is a small molecule with a molecular weight of approximately 373.35 (estimated from the molecular formula C23H19N3O2).
|
| Toxicity/Toxicokinetics |
No specific toxicity data is publicly available for CYM-50260. In cell-based assays, the compound shows activity at nanomolar concentrations, suggesting a potential therapeutic window. The compound is for research use only and is not intended for human therapeutic applications. No systemic toxicity studies have been reported.
|
| References |
|
| Additional Infomation |
CYM-50260 is a potent and selective S1P4 receptor agonist with an EC50 of 45 nM. Its molecular formula is C23H19N3O2 and its molecular weight is approximately 373.35. The compound is also known as CYM50260. It is a valuable research tool for studying the role of S1P4 signaling in platelet function, immune regulation, and other physiological processes. It is not approved for clinical use.
|
| Molecular Formula |
C14H11CL3FNO2
|
|---|---|
| Molecular Weight |
350.5954
|
| Exact Mass |
348.984
|
| CAS # |
1355026-60-6
|
| PubChem CID |
44620894
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.969
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
21
|
| Complexity |
314
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
FHPOTBQOUBMMCI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C14H11Cl3FNO2/c15-9-1-3-12(11(16)7-9)20-5-6-21-13-4-2-10(8-18)19-14(13)17/h1-4,7H,5-6,8H2
|
| Chemical Name |
2-chloro-3-[2-(2,4-dichlorophenoxy)ethoxy]-6-(fluoromethyl)pyridine
|
| Synonyms |
CYM50260; CYM 50260; CYM-50260
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~356.53 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8523 mL | 14.2613 mL | 28.5225 mL | |
| 5 mM | 0.5705 mL | 2.8523 mL | 5.7045 mL | |
| 10 mM | 0.2852 mL | 1.4261 mL | 2.8523 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
