2. Immunology/Inflammation
  3. Macrophage migration inhibitory factor (MIF) COX
  4. Iguratimod

Iguratimod  (Synonyms: T614)

Cat. No.: HY-17009 Purity: 99.93%
COA 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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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
5 mg USD 55 In-stock
10 mg USD 77 In-stock
50 mg USD 275 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Iguratimod Related Antibodies

Top Publications Citing Use of Products

    Iguratimod purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2019 Nov;119:109455.  [Abstract]

    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 MedChemExpress. Usage Cited in: Biomed Pharmacother. 2019 Nov;119:109455.  [Abstract]

    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 MedChemExpress. Usage Cited in: Biomed Pharmacother. 2019 Nov;119:109455.  [Abstract]

    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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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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].

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

    Iguratimod Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    374.37

    Appearance

    Solid

    Formula

    C17H14N2O6S
    CAS No.
    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 2 years
    -20°C 1 year
    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 MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.93%

    COA (249 KB) LCMS (263 KB)

    Handling Instructions (2659 KB)
    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
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    Iguratimod Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Iguratimod123663-49-0T614T 614T-614Macrophage migration inhibitory factor (MIF)COXCyclooxygenaseInhibitorinhibitorinhibit

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