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Esonarimod (Synonyms: KE-298)

目录号: HY-19440
产品使用指南

Esonarimod 是一种抗风湿药物。

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Esonarimod Chemical Structure

Esonarimod Chemical Structure

CAS No. : 101973-77-7

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥3392 In-stock
1 mg ¥1100 In-stock
5 mg ¥3300 In-stock
10 mg ¥5000 In-stock
50 mg ¥15000 In-stock
100 mg ¥21000 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

Esonarimod is an antirheumatic drug.

In Vitro

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].

In Vivo

After repeated oral administration of Esonarimod (14C-KE-298), the radioactivity decreases rapidly and no tendency towards accumulation is found[2].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 3.5671 mL 17.8355 mL 35.6710 mL
5 mM 0.7134 mL 3.5671 mL 7.1342 mL
10 mM 0.3567 mL 1.7835 mL 3.5671 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

For 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Esonarimod (14C-KE-298) is dissolved in EtOH solution and adjusted to pH 9 to 11 with 0.4 M NaOH.

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

280.34

Formula

C₁₄H₁₆O₄S

CAS No.

101973-77-7

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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产品名称:
Esonarimod
目录号:
HY-19440
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