| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
S1P1-IN-Ex26 targets the sphingosine-1-phosphate receptor 1 (S1P1), a G protein-coupled receptor that plays a critical role in lymphocyte trafficking. S1P1 signaling is required for the egress of lymphocytes from lymph nodes and other lymphoid organs. By antagonizing S1P1, the compound inhibits lymphocyte egress, leading to immunosuppression.
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| ln Vitro |
Excellent selectivity for S1P1 over other sphingosine-1-phosphate receptors is demonstrated by Ex26 (0-10 μM; 1 hour) treatment [1].
S1P1-IN-Ex26 is a potent and selective antagonist of S1P1. It has high affinity for S1P1 and selectivity over other S1P receptors. In vitro, it inhibits S1P-induced S1P1 activation and downstream signaling. Specific IC50 or Ki values are not detailed in the available literature. |
| ln Vivo |
Treatment with ex26 (ip; 3 mg/kg; once daily; 3 d) suppresses lymphocyte and thymocyte efflux and interferes with S1P1 signaling [1]. Through S1P1 antagonistic action, ex26 (ip; 30 mg/kg; once daily; 15 days) therapy ameliorates experimental autoimmune encephalomyelitis [1].
S1P1-IN-Ex26 has been shown to modulate immune responses in vivo by inhibiting lymphocyte egress from lymphoid organs. This leads to lymphopenia and immunosuppression. It has been studied in animal models of autoimmune diseases and transplantation for its potential therapeutic applications. |
| Enzyme Assay |
The in vitro activity of S1P1-IN-Ex26 is assessed using radioligand binding assays. Membrane preparations from cells expressing S1P1 are incubated with a labeled S1P ligand in the presence of various concentrations of the compound. The Ki values are calculated from displacement curves. Selectivity against other S1P receptors is confirmed.
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| Cell Assay |
Cell viability assay [1]
Cell Types: U2OS cells and Chinese hamster ovary cells Tested Concentrations: 0-10 μM Incubation Duration: 1 hour Experimental Results: Confirmed to be a potent and selective antagonist of S1P1 (IC50=0.93 nM). The antagonist activity of S1P1-IN-Ex26 is assessed in functional cell-based assays. Cells expressing S1P1 are treated with S1P in the presence or absence of the compound. Receptor activation is measured by assessing the inhibition of forskolin-stimulated cAMP accumulation (S1P1 is coupled to Gi) or by measuring other downstream signaling events. IC50 values are calculated. |
| Animal Protocol |
Animal/Disease Models: 8weeks old male C57Bl/6J mice [1]
Doses: 3 mg/kg Route of Administration: intraperitoneal (ip) injection; 3 mg/kg; one time/day; 3 days Experimental Results: low dose induction of lymphocyte isolation, treatment for 2 hrs (hrs (hours)) The post-ED50 is 0.06 mg/kg. Resulting in significant retention of T and B cells in lymph nodes and a significant decrease in T and B cells in the spleen. Animal/Disease Models: 8weeks old male C57Bl/6J mice, induced experimental autoimmune encephalomyelitis [1] Doses: 30 mg/kg Route of Administration: intraperitoneal (ip) injection; intraperitoneal (ip) injection. 30 mg/kg; one time/day; 15 days Experimental Results: Inhibited lymphocyte infiltration and spinal cord white matter destruction in mice euthanized at the end of the experiment. S1P1-IN-Ex26 has been evaluated in animal models of autoimmune diseases and transplantation. In these studies, the compound is typically administered to animals, and its effects on lymphocyte counts, immune responses, and disease progression are assessed. |
| ADME/Pharmacokinetics |
S1P1-IN-Ex26 has a molecular weight and formula that are not detailed in the available literature. It is a potent and selective S1P1 antagonist. Purity is typically ≥98%. The compound is soluble in DMSO. Storage is recommended at -20°C. It is a research compound for studying S1P1 function and potential therapeutic applications in immune-mediated diseases.
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| Toxicity/Toxicokinetics |
S1P1-IN-Ex26 is a research compound and its full toxicological profile is not detailed in the available literature. As an S1P1 antagonist, it causes lymphopenia and immunosuppression, which can increase the risk of infections. Its safety profile would be evaluated in preclinical toxicology studies for its development as a therapeutic agent.
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| References | |
| Additional Infomation |
S1P1-IN-Ex26 (CAS#: 1233332-37-0) is a potent and selective sphingosine-1-phosphate receptor 1 (S1P1) antagonist. It inhibits lymphocyte egress from lymphoid organs by blocking S1P1 signaling, leading to immunosuppression. It is a valuable research tool for studying S1P1 function in immune cell trafficking, inflammation, and autoimmune diseases. It has potential therapeutic applications in transplantation and autoimmune disorders.
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| Molecular Formula |
C28H28CLFN2O3
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| Molecular Weight |
494.984930038452
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| Exact Mass |
494.177
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| CAS # |
1233332-37-0
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| PubChem CID |
59393740
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
634.3±55.0 °C at 760 mmHg
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| Flash Point |
337.4±31.5 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.639
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| LogP |
6.12
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
35
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| Complexity |
765
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YVHNBORUVLWCKF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H28ClFN2O3/c1-15-11-19(5-7-23(15)29)18(4)31-21-6-8-24(30)22(14-21)20-12-16(2)25(17(3)13-20)26(33)32-28(9-10-28)27(34)35/h5-8,11-14,18,31H,9-10H2,1-4H3,(H,32,33)(H,34,35)
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| Chemical Name |
1-[[4-[5-[1-(4-chloro-3-methylphenyl)ethylamino]-2-fluorophenyl]-2,6-dimethylbenzoyl]amino]cyclopropane-1-carboxylic acid
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| 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 | 2.0203 mL | 10.1014 mL | 20.2028 mL | |
| 5 mM | 0.4041 mL | 2.0203 mL | 4.0406 mL | |
| 10 mM | 0.2020 mL | 1.0101 mL | 2.0203 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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