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[CAS NO. 123663-49-0] Iguratimod
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-17009 |
| Brand: | MCE |
| CAS: | 123663-49-0 |
Overview
| MDL | MFCD00882374 |
|---|---|
| Molecular Weight | 374.37 |
| Molecular Formula | C17H14N2O6S |
| SMILES | O=C1C2=CC(OC3=CC=CC=C3)=C(C=C2OC=C1NC([H])=O)NS(=O)(C)=O |
3 Publications Citing Use of MCE
Summary
Iguratimod is an antirheumatic agent, acts as an inhibitor of COX-2 , with an IC 50 of 20 μM (7.7 μg/mL), but shows no effect on COX-1 . Iguratimod also inhibits macrophage migration inhibitory factor ( MIF ) with an IC 50 of 6.81 μM.
IC50 & Target
|
COX-2 20 μM (IC 50 ) |
MIF 6.81 μM (IC 50 ) |
In Vitro
Iguratimod (T-614) is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC 50 of 20 μM (7.7 μg/mL), but shows no effect on COX-1. Iguratimod (0.1, 1, 10 μg/mL) inhibits bradykinin-stimulated PGE2 release from fibroblasts. Iguratimod suppresses the COX activity from bradykinin stimulated fibroblasts in a concentration-dependent manner, with an IC 50 of 48 μg/mL. Iguratimod (10 and 30 μg/mL) also dose-dependently inhibits COX-2 mRNA levels [1] . In addition, Iguratimod potently inhibits macrophage migration inhibitory factor (MIF) with an IC 50 of 6.81 μM. Iguratimod is synergetic with glucocorticoids in vitro [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Iguratimod (5 or 20 mg/kg) shows analgesic effect, significantly improves the pain withdrawal threshold of the left hind paw in dose-dependent manner in rats. Iguratimod (5 or 20 mg/kg) reduces the elevation of pERK1/2 and c-Fos in the spinal cord induced by cancer cell inoculation. Iguratimod also dose-dependently decreases the IL-6 levels in rats. In Iguratimod-treated rats, the activity of osteoclasts is weaker than the control group [2] . Iguratimod (20 mg/kg i.p.) shows significantly increased survival in BALB/c mice that are vulnerable to endotoxemia, and attenuates TNFα release measured in serum isolated 90 min post-LPS administration in wild-type C57BL/6 mice [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03855007 | Qilu Hospital of Shandong University |
Arthritis, Rheumatoid
|
January 1, 2016 | Phase 4 |
| NCT01554917 | Jiangsu Simcere Pharmaceutical Co., Ltd. |
Rheumatoid Arthritis
|
May 2012 | Phase 4 |
| NCT01850966 | Eisai Co., Ltd.|Eisai Inc. |
Rheumatoid Arthritis
|
September 12, 2012 | |
| NCT03054545 | RenJi Hospital |
Lupus Nephritis
|
May 8, 2017 | Not Applicable |
| NCT03023592 | Peking Union Medical College Hospital |
Sjogren´s Syndrome
|
February 2017 | Phase 1|Phase 2 |
| NCT00965757 | Eisai Co., Ltd.|FUJIFILM Toyama Chemical Co., Ltd.|Eisai Inc. |
Rheumatoid Arthritis
|
July 31, 2009 | Phase 3 |
| NCT04928066 | Qilu Hospital of Shandong University |
Arthritis, Rheumatoid
|
March 1, 2020 | Phase 4 |
| NCT02275299 | Jiangsu Simcere Pharmaceutical Co., Ltd. |
Rheumatoid Arthritis
|
September 2013 | Phase 4 |
| NCT05302024 | Peking University People´s Hospital |
Immune Thrombocytopenia
|
March 22, 2022 | Phase 2 |
| NCT05281068 | Peking University People´s Hospital|Beijing Hospital|China-Japan Friendship Hospital|Beijing Friendship Hospital|The First Affiliated Hospital of Zhengzhou University|First Affiliated Hospital of Chongqing Medical University|Shanxi Bethune hospital, Shanxi, China |
ITP|Immune Thrombocytopenia
|
September 1, 2021 | Phase 2 |
| NCT05626348 | Qilu Hospital of Shandong University |
Arthritis, Rheumatoid
|
December 22, 2021 | Phase 4 |
| NCT05216757 | Peking University People´s Hospital |
Hand Osteoarthritis|Inflammatory Arthritis
|
March 2022 | Phase 2|Phase 3 |
| NCT02936375 | RenJi Hospital |
Lupus Nephritis
|
September 7, 2017 | Phase 2 |
| NCT03368274 | Wen Zhang|Peking Union Medical College Hospital |
IgG4-related Disease
|
September 1, 2017 | Phase 4 |
| NCT04830644 | Jiangsu Simcere Pharmaceutical Co., Ltd. |
Primary Sjögren Syndrome
|
March 22, 2021 | Phase 2 |
| NCT01548001 | Jiangsu Simcere Pharmaceutical Co., Ltd. |
Rheumatoid Arthritis
|
May 2012 | Phase 4 |
| NCT01893151 | Jiangsu Simcere Pharmaceutical Co., Ltd. |
Rheumatoid Arthritis
|
July 2012 | Phase 4 |
| NCT04981145 | Second Affiliated Hospital, School of Medicine, Zhejiang University |
Primary Sjögren´s Syndrome
|
January 14, 2022 | Phase 4 |
| NCT02839941 | The First Affiliated Hospital with Nanjing Medical University |
Kidney Transplantation
|
August 2016 | Not Applicable |
| NCT04515706 | RenJi Hospital |
Systemic Sclerosis, Diffuse
|
January 1, 2021 | Not Applicable |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 33.33 mg/mL ( 89.03 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.6712 mL | 13.3558 mL | 26.7115 mL |
| 5 mM | 0.5342 mL | 2.6712 mL | 5.3423 mL |
| 10 mM | 0.2671 mL | 1.3356 mL | 2.6712 mL |
-
1.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (6.68 mM); Suspended solution; Need ultrasonic
References
- [1] Tanaka K, et al. T-614, a novel antirheumatic drug, inhibits both the activity and induction of cyclooxygenase-2 (COX-2) in cultured fibroblasts. Jpn J Pharmacol. 1995 Apr;67(4):305-14.
- [2] Sun Y, et al. Anti-rheumatic drug iguratimod protects against cancer-induced bone pain and bone destruction in a rat model. Oncol Lett. 2017 Jun;13(6):4849-4856.
- [3] Iguratimod, et al. Identification of Iguratimod as an Inhibitor of Macrophage Migration Inhibitory Factor (MIF) with Steroid-sparing Potential. J Biol Chem. 2016 Dec 16;291(51):26502-26514.
Synonyms
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