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  3. Iguratimod

Iguratimod (Synonyms: T614)

Cat. No.: HY-17009 Purity: 99.97%
Handling Instructions

Iguratimod is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC50 of 20 μM (7.7 μg/mL), but shows no effect on COX-1. Iguratimod also inhibits macrophage migration inhibitory factor (MIF) with an IC50 of 6.81 μM.

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

Iguratimod Chemical Structure

Iguratimod Chemical Structure

CAS No. : 123663-49-0

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 70 In-stock
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50 mg USD 250 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Iguratimod purchased from MCE. Usage Cited in: Biomed Pharmacother. 2019 Sep 18;119:109455. 

    Effects of T-614 on pro-inflammatory cytokines in SAP in mice. Con, control group; SAP, cerulein plus LPS group; T-614, SAP and Iguratimod treatment group. Serum IL-6, TNF-α and IL-1β expression were measured by ELISA in three different groups. IL-6, TNF-α and IL-1β mRNA levels in pancreatic tissue are detected by real-time PCR.

    Iguratimod purchased from MCE. Usage Cited in: Biomed Pharmacother. 2019 Sep 18;119:109455. 

    Effects of T-614 on COX2 expression in pancreas. Con, control group; SAP, cerulein plus LPS group; T-614, SAP and Iguratimod treatment group. COX-2 level by western blotting. COX2 protein relative to GAPDH level.

    Iguratimod purchased from MCE. Usage Cited in: Biomed Pharmacother. 2019 Sep 18;119:109455. 

    Effects of T-614 on NF-κB pathway and NLRP3 pathway in SAP in mice. The immunohistochemical detection of p-p65 and NLRP3 in the pancreas tissues.

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    Description

    Iguratimod is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC50 of 20 μM (7.7 μg/mL), but shows no effect on COX-1. Iguratimod also inhibits macrophage migration inhibitory factor (MIF) with an IC50 of 6.81 μM.

    IC50 & Target[1][3]

    COX-2

    20 μM (IC50)

    MIF

    6.81 μM (IC50)

    In Vitro

    Iguratimod (T-614) is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC50 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 IC50 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 IC50 of 6.81 μM. Iguratimod is synergetic with glucocorticoids in vitro[3].

    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].

    Clinical Trial
    Molecular Weight

    374.37

    Formula

    C₁₇H₁₄N₂O₆S

    CAS No.

    123663-49-0

    SMILES

    O=C1C2=CC(OC3=CC=CC=C3)=C(C=C2OC=C1NC([H])=O)NS(=O)(C)=O

    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)

    H2O : < 0.1 mg/mL (insoluble)

    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 provided by MCE.
    References
    Cell Assay
    [3]

    Briefly, human Raji B cells are plated at a density of 0.5 × 104 cells/well in a 96-well plate and synchronized by incubation for 24 h in RPMI 1640 medium supplemented with 0.1-0.5% FBS. Synchronized cells are pretreated with Iguratimod or vehicle for 30 min prior to stimulation with macrophage migration inhibitory factor (MIF) for 24 h. At 20 h BrdU is added to cells and quantified using a BrdU Cell proliferation assay kit[3].

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

    Animal Administration
    [3]

    Mice[3]
    Endotoxemia is induced by intraperitoneal injection of LPS from E. coli O111:B4. In BALB/c animals, 5 mg/kg LPS is used as a lethal dose for survival experiments; animals are treated with Iguratimod (20 mg/kg i.p.) 0.5 h prior to LPS, 6 h after LPS, and then once daily for 3 days and monitored for survival over 2 weeks. In C57BL/6 animals, 20 mg/kg LPS is used as non-lethal dose for plasma cytokine experiments; animals are pretreated with Iguratimod (20 mg/kg i.p.) twice, one dose each at 2 and 0.5 h prior to LPS administration, and euthanized at 90 min post-LPS by CO2 asphyxiation with cervical dislocation. Blood is collected by cardiac puncture and allowed to clot 20 min at room temperature and 20 min at 4°C; sera are isolated by centrifugation at 300 × g for 10 min and stored at −20°C for further analysis by TNFα ELISA (1:3 dilution)[3].

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

    References

    Purity: 99.97%

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    Keywords:

    IguratimodT614T 614T-614COXCyclooxygenaseInhibitorinhibitorinhibit

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    Product Name:
    Iguratimod
    Cat. No.:
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