[CAS NO. 123663-49-0] Iguratimod

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PRODUCTS SPECIFICATIONS [123663-49-0]

Catalog

HY-17009

Brand

MCE

CAS

123663-49-0

DESCRIPTION [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

For research use only. We do not sell to patients.

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

In Vitro:

DMSO : 33.33 mg/mL ( 89.03 mM ; Need ultrasonic)

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

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

* All of the co-solvents are available by MCE.

References

Synonyms

Methanesulfonamide, N-[3-(formylamino)-4-oxo-6-phenoxy-4H-1-benzopyran-7-yl]-

N-[3-(Formylamino)-4-oxo-6-phenoxy-4H-1-benzopyran-7-yl]methanesulfonamide

T 614

3-Formylamino-7-methylsulfonylamino-6-phenoxy-4H-1-benzopyran-4-one

Iguratimod

N-[3-(Formylamino)-4-oxo-6-phenoxy-4H-chromen-7-yl]methanesulfonamide

T 614 (antiinflammatory)

Careram

Kolbet