Esonarimod (KE-298) (Synonyms: KE-298) |
| Katalog-Nr.GC31933 |
Esonarimod (KE-298) (KE-298) ist ein Antirheumatikum.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 101973-77-7
Sample solution is provided at 25 µL, 10mM.
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Esonarimod is an antirheumatic drug.
Esonarimod (KE-298) (10 to 300 μg/mL) suppresses the production of NO by RAW264.7 cells in a dose dependent manner. The IC50 of Esonarimod is 117.5 μg/mL. Esonarimod does not affect cellular viability at these tested doses. Esonarimod has no direct effect on NOS activity in cell-free extracts of RAW264.7 cells[1].
After repeated oral administration of Esonarimod (14C-KE-298), the radioactivity decreases rapidly and no tendency towards accumulation is found[2].
[1]. Inoue T, et al. KE-298 and its active metabolite KE-758 suppress nitric oxide production by murine macrophage cells and peritoneal cells from rats with adjuvant induced arthritis. J Rheumatol. 2001 Jun;28(6):1229-37. [2]. Hasegawa M, et al. Formation of a disulfide protein conjugate of the SH-group-containing metabolite (M-I) ofesonarimod (KE-298) and its elimination in rats. J Pharm Pharmacol. 2002 Apr;54(4):493-8.
Kinase experiment: | Enzyme activity of NOS is determined using an assay kit for NOS activity. Briefly, the lysate from RAW264.7 cells (a protein concentration of 37.5 μg/200 μL) is incubated for 3 h at 37°C with 100 mM of L-arginine in the presence of Esonarimod (KE-298) and the conversion of L-arginine to nitrite is monitored. The nitrite generated in the reaction mixture is assayed using Griess reagent[1]. |
Cell experiment: | in vitro experiment, Esonarimod (KE-298) is dissolved in ethanol and diluted with culture medium or distilled water.--> RAW264.7 cells are used in this study. For NO production, RAW264.7 cells [2×105/0.2 mL of RPMI-1640 supplemented by 10% heat inactivated fetal bovine serum (FBS), penicillin G (100 U/mL), and streptomycin (100 μg/mL)] are stimulated with 100 ng/mL of Escherichia coli 026:B6 lipopolysaccharide in the presence of Esonarimod (KE-298) (0, 10, 30, 100, 200, 300 μg/mL) in 96 well plates and incubated 24 h at 37°C in an atmosphere of 5% CO2 in air. After incubation, the supernatants are collected and assayed for nitrite (NO2-) instead of NO[1]. |
Animal experiment: | Seven-week-old male Wistar rats are used in this study. The animals are fasted overnight before dosing and for up to 4 h after dosing, except for the study on tissue distribution after repeated oral administration. The rats are grouped, three or four rats per group. Esonarimod (14C-KE-298) is administered orally by gastric intubation in a dose of 5 mg/kg once daily for 21 days. At 20 min, 24 h or 21 days after dosing with Esonarimod, the rats are anaesthetized with ether and blood samples are collected from the femoral aorta into heparinized containers. The liver, kidney, lung, aorta and skin are excised and weighed. Tissues (except aorta) are homogenized with ice-cold physiological saline to yield a 20% homogenate[2]. |
References: [1]. Inoue T, et al. KE-298 and its active metabolite KE-758 suppress nitric oxide production by murine macrophage cells and peritoneal cells from rats with adjuvant induced arthritis. J Rheumatol. 2001 Jun;28(6):1229-37. | |
| Cas No. | 101973-77-7 | SDF | |
| Überlieferungen | KE-298 | ||
| Canonical SMILES | CC1=CC=C(C(CC(CSC(C)=O)C(O)=O)=O)C=C1 | ||
| Formula | C14H16O4S | M.Wt | 280.34 |
| Löslichkeit | DMSO : 100 mg/mL (356.71 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.5671 mL | 17.8355 mL | 35.671 mL |
| 5 mM | 713.4 μL | 3.5671 mL | 7.1342 mL |
| 10 mM | 356.7 μL | 1.7835 mL | 3.5671 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Quality Control & SDS
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- Purity: >99.50%
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- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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