| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
S1PR1/S1PR5 agonist-1 effectively activated S1PR1 in CHO-K1 cells that stably expressed S1PR1/Gα16, with an EC50 of 40.0 ± 2.5 nM [1]. S1PR1/S1PR5 agonist-1 effectively activated S1PR5 in cells that stably expressed S1PR5/Gα16/CHO-K1, with an EC50 of 22.9 ± 0.5 nM [1].
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|---|---|
| ln Vivo |
S1PR1/S1PR5 agonist-1 (3 mg/kg; orally) protected cardiac function in male C57BL/6J mice without showing significant negative chronotropic effects [1]. S1PR1/S1PR5 agonist-1 (3 mg/kg; orally; once daily; for 10 days) significantly reduced dextran sulfate-induced colitis in male C57BL/6J mice, with better efficacy than 50 mg/kg 5-aminosalicylic acid [1].
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| Animal Protocol |
Animal/Disease Models:C57BL/6J mice (male, 10 weeks old, SPF grade) [1]
Doses: 3 mg/kg Route of Administration: Oral Experimental Results: Cardiac function was maintained during the 72-hour evaluation period, with ejection fraction and fractional shortening remaining normal. No significant negative chronotropic effects were observed. A transient increase in baseline heart rate was induced on day 3, which partially subsided after the third dose. Animal/Disease Models:C57BL/6J mice (male, DSS-induced colitis model) [1] Doses: 3 mg/kg Route of Administration: Oral; once daily; 10 days Experimental Results: Compared with the solvent group, this study significantly improved acute colitis, reduced weight loss, decreased disease activity index score, and increased colon length. The efficacy was superior to 50 mg/kg 5-aminosalicylic acid (5-ASA). Histopathological analysis showed improved epithelial structure, reduced ulceration, and reduced inflammatory infiltration. Immunofluorescence staining showed reduced infiltration of F4/80 positive macrophages. Immunohistochemistry showed reduced recruitment of Ly-6G positive neutrophils. Hematological analysis showed a decrease in peripheral blood lymphocyte count, consistent with S1PR1-mediated lymphocyte retention. |
| References |
| Molecular Formula |
C29H28N4O4
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|---|---|
| Molecular Weight |
496.56
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
CC(OC(C=CC(C1=NC(C2=CC=C(C3=C2C=CC=C3)CN4C[C@@H]([C@H](C4)C)C(O)=O)=NO1)=C5)=C5C#N)C
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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 | 2.0139 mL | 10.0693 mL | 20.1386 mL | |
| 5 mM | 0.4028 mL | 2.0139 mL | 4.0277 mL | |
| 10 mM | 0.2014 mL | 1.0069 mL | 2.0139 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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