Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
IC50: 8.26 μM (RAGE), 31.09 nM (SERT)[1]
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ln Vitro |
Compound 12 (RAGE/SERT-IN-1; 1–20 μM; 24 hours) has no discernible effect on SH-SY5Y cell viability[1].
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ln Vivo |
RAGE/SERT-IN-1 (0-10 μM; 60 min) does not appear to inhibit major CYP enzymes and has decent liver microsomal stability[1]. At 100 mg/kg, RAGE/SERT-IN-1 (100 and 200 mg/kg; IP; single dosage) does not result in the mortality of mice or significantly alter the organ-to-body weight ratio[1]. In the tail suspension test, RAGE/SERT-IN-1 (60 mg/kg; PO; single dosage) dramatically shortens the immobility period[1]. In mice, RAGE/SERT-IN-1 (single dosage; 60 mg/kg PO, 10 mg/kg IV) shows reasonable pharmacokinetic characteristics[1]. RAGE/SERT-IN-1 pharmacokinetic parameters in male ICR mice[1]. AUC0-∞ (ng/mL·h) 24684 23653 CL (mL/min/kg) 7.09 VSS (L/kg) 1037 F (%) 17.1 PO (60 mg/kg) IV (10 mg/kg) T1/2 (h) 5.55 3.46 Cmax (ng/mL) 4935 51745
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Cell Assay |
Cell Cytotoxicity Assay
Cell Types: SH-SY5Y[1] Tested Concentrations: 1, 5, 10 and 20 μM Incubation Duration: 24 hrs (hours) Experimental Results: Did not affect cell viability at concentrations of 1, 5, and 10 μM, and only a slight decrease in cell viability at the concentration of 20 μM was observed with the viability still above 80%. |
Animal Protocol |
Animal/Disease Models: Male ICR mice (24-26 g)[1]
Doses: 100mg/kg and 200mg/ kg Route of Administration: IP; single (observed for 2 weeks) Experimental Results: All mice were survived and no significant changed in the ratio of organ-to-body weight at a dose of 100 mg/kg. Animal/Disease Models: Male ICR mice[1] Doses: 60 mg/kg Route of Administration: PO; single dosage Experimental Results: Dramatically decreased the immobility time in tail suspension test. Animal/Disease Models: Male ICR mice[1] Doses: 60 mg/kg for PO, 10 mg/kg for IV Route of Administration: PO and IV; single dosage Experimental Results: demonstrated acceptable pharmacokinetic/PK properties in mice. |
References |
[1]. Zhang C, Wang L, Xu Y, et al. Discovery of novel dual RAGE/SERT inhibitors for the potential treatment of the comorbidity of Alzheimer's disease and depression. Eur J Med Chem. 2022;236:114347.
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Molecular Formula |
C38H41CLN4OS
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Molecular Weight |
637.28
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CAS # |
2766739-35-7
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Appearance |
Typically exists as solids (or liquids in special cases) 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 | 1.5692 mL | 7.8458 mL | 15.6917 mL | |
5 mM | 0.3138 mL | 1.5692 mL | 3.1383 mL | |
10 mM | 0.1569 mL | 0.7846 mL | 1.5692 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.