| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Molecular docking studies of S1P1 agonist 7 (compound 28) showed that it exhibited a 4.51-fold β-repressor bias relative to Fingolimod, with a G protein signaling pathway EC50 of 12.7 nM and a β-repressor recruitment EC50 of 3.23 nM [1]. S1P1 agonist 7 (1-10 µM, 15-60 min) showed high stability in liver microsomes of all humans, rats and mice, and had no significant inhibitory effect on most CYP isoenzymes at a concentration of 10 µM [1]. S1P1 agonist 7 (serially diluted from a starting concentration of 100 μM, 90 min) showed high selectivity for the S1P1 receptor in Chem-4/G15 and CHO-K1 EDG1 cell models, with an EC50 of 0.014 μM for G protein signaling and 0.0023 μM for β-repressor recruitment, and showed only weak activity against the S1P5 receptor [1]. S1P1 agonist 7 (0.041–10 μM, 2 min) did not induce any observable changes in peak frequency or beat rate in human iPSC-derived cardiomyocytes, even at the highest tested concentration [1].
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| ln Vivo |
S1P1 agonist 7 (1, 3 and 10 mg/kg, by gavage, or a single spray) reduced peripheral blood replication counts in C57BL/6N mice [1]. S1P1 agonist 7 (10 mg/kg, by gavage, once daily for 23 days) showed strong protective effects in a MOG35-55-induced EAE mouse model, blocking its disease effects, inhibiting disease progression and attenuating associated pathological damage [1].
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| Animal Protocol |
Animal/Disease Models: Female C57BL/6N mice (8 weeks old) immunized with MOG/CFA emulsion and received PTX on two consecutive days to induce EAE[1]
Doses: 10 mg/kg Route of Administration: i.g., daily for 23 days Experimental Results: Delayed disease onset and reduced symptom severity, as indicated by lower cumulative and mean maximum clinical scores. Maintained its prophylactic effect until the peak of disease severity, which occurred around 17 dpi. Prevented body weight loss and lowered disease incidence in EAE mice, indicating a protective effect. Moderated disease progression, and led to a steady reduction in symptom severity until 34 dpi, demonstrating a moderate therapeutic effect comparable to that of Siponimod. Significantly reduced the cumulative clinical score from 19 dpi (the peak of EAE) to 34 dpi. Prevented body weight loss compared to the vehicle-treated group. Markedly reduced demyelination in the spinal cord's dorsal column and ventral white matter. Reduced immune cell infiltration and partially preserved myelin integrity. Animal/Disease Models: Female C57BL/6N mice (8 weeks old)[1] Doses: 1, 3, and 10 mg/kg Route of Administration: i.g., single dose Experimental Results: Reduced PLC to 24.4 % of baseline at 4 h post administration, outperforming Fingolimod (36.3 %). Promoted a rapid recovery of PLCs to 70.8 % of baseline within 28 hours, in contrast to Fingolimod, which causes prolonged lymphopenia. Produced a rapid reduction in lymphocyte counts to approximately 40 % of baseline at 3 h post administration and achieved maximal suppression at the 3 and 10 mg/kg doses by 6 h post administration, while triggering an early rebound in the 1 mg/kg group by the same time, suggesting the onset of recovery. Elicited a stronger pharmacodynamic response at 3 and 10 mg/kg, and permitted full lymphocyte recovery in all groups within 24 hours. |
| References |
| Molecular Formula |
C23H22N2O5
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|---|---|
| Molecular Weight |
406.43
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| Appearance |
Typically exists as solids at room temperature
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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 | 2.4604 mL | 12.3022 mL | 24.6045 mL | |
| 5 mM | 0.4921 mL | 2.4604 mL | 4.9209 mL | |
| 10 mM | 0.2460 mL | 1.2302 mL | 2.4604 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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