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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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S-methyl-KE-298 is an active metabolite of KE-298, which is an inhibitor of matrix metalloproteinase (MMP-1) production from rheumatoid arthritis (RA) synovial cells.
ln Vitro |
The methyl conjugate of deacetyl-KE-298 in plasma is known as S-Methyl-KE-298 [1]. In vitro protein binding of KE-298 in rats (>97%), dogs (>89%), and human plasma (>99%), and its plasma metabolites deacetyl-KE-298 (M-1) and S-methyl-KE-298 (M-2), respectively [2]. While KE-298 does not influence IL-1β-induced tissue inhibitor of metalloproteinase 2 (TIMP-2) secretion by rheumatoid synoviocytes, it does block IL-1β-induced pro-MMP-2 activation and MT1-MMP expression. By altering the transcription factor AP-1, KE-298 prevents rheumatoid arthritis (RA) synoviocytes from producing MMP-1. MT1-MMP expression at basal levels is inhibited by KE-298 in unstimulated rheumatoid synoviocytes [3].
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References |
[1]. Yoshida H, et al. Identification of metabolites of KE-298, a new antirheumatic drug, and its physiological properties in rats. Biol Pharm Bull. 1996 Mar;19(3):424-9.
[2]. Endo H, et al. Stereoselectivity and species difference in plasma protein binding of KE-298 and its metabolites. Biol Pharm Bull. 2001 Jul;24(7):800-5. [3]. Honda S, et al. Expression of membrane-type 1 matrix metalloproteinase in rheumatoid synovial cells. Clin Exp Immunol. 2001 Oct;126(1):131-6. |
Molecular Formula |
C₁₃H₁₆O₃S
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Molecular Weight |
252.33
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CAS # |
143584-75-2
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
S(C([H])([H])[H])C([H])([H])C([H])(C(=O)O[H])C([H])([H])C(C1C([H])=C([H])C(C([H])([H])[H])=C([H])C=1[H])=O
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Synonyms |
S-methyl-KE-298S-methyl-KE298
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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) |
DMSO : ~100 mg/mL (~396.31 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.9631 mL | 19.8153 mL | 39.6306 mL | |
5 mM | 0.7926 mL | 3.9631 mL | 7.9261 mL | |
10 mM | 0.3963 mL | 1.9815 mL | 3.9631 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.