| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
GSK235 (compound 21) (1 μM, 0.61 μM; 1 h, 24 h) exhibits potent and highly selective inhibition of ERAP1 and ERAAP in human and mouse enzymes [1]. GSK235 showed a pIC50 value of 7.25 in the HeLa antigen presentation assay [1]. GSK235 (1 µM; 30 days) affected a variety of immune peptides in CT26 tumor cells. A significant increase in peptide chain length was observed; for example, a significant increase in decapeptides and 11capeptides was accompanied by a decrease in 9capeptides and 8capeptides [1]. GSK235 has no activity against hERG channels [1].
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|---|---|
| ln Vivo |
GSK235 (compound 21) (30, 90, 270 mg/kg, adjacent, twice daily for 17 days) reduced tumor growth and modulated the immune peptidome in a dose-dependent manner in the CT26 homology model [1]. GSK235 (30, 90, 270 mg/kg, face, twice daily from day 18 to day 36) reduced arthritis scores and immune activation in a dose-stimulated collagen-induced arthritis (CIA) subject model without evidence of autoimmune protection [1].
|
| Animal Protocol |
Animal/Disease Models: Female BALB/c (6-8 weeks old) were inoculated subcutaneously in the right hind flank with 5x104 CT26 cells[1]
Doses: 30 mg/kg, 90 mg/kg, 270 mg/kg Route of Administration: Oral; twice daily (BID); for 17 days Experimental Results: Observed with significant reduction in tumor volume by termination of the study, day 17, at the highest dose (270 mg/kg) and no significant dose-dependent body-weightchanges were observed. Animal/Disease Models: Male DBA/1OlaHsd (6-7 weeks old) (Collagen-induced arthritis (CIA) model)[1] Doses: 30 mg/kg, 90 mg/kg, 270 mg/kg Route of Administration: Oral; twice daily (BID); from day 18 to day 36 Experimental Results: Showed a dose-dependent reduction in arthritis scores, with the highest dose (270 mg/kg) achieving a reduction comparable to the TNF inhibitor Enbrel. Also reduced anti-collagen type II IgG levels, IL-12p40, and IL-6 levels, and decreased MHC-I expression on B cells and cDCs. No exacerbation of autoimmune responses was observed. |
| References |
| Molecular Formula |
C21H30N4O3
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|---|---|
| Molecular Weight |
386.49
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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 | 2.5874 mL | 12.9369 mL | 25.8739 mL | |
| 5 mM | 0.5175 mL | 2.5874 mL | 5.1748 mL | |
| 10 mM | 0.2587 mL | 1.2937 mL | 2.5874 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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