2. Apoptosis Immunology/Inflammation
  3. TNF Receptor Interleukin Related IFNAR
  4. Roquinimex

Roquinimex  (Synonyms: Linomide; FCF89; ABR212616)

Cat. No.: HY-13743 Purity: 99.69%
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Roquinimex (Linomide) is an orally active immunomodulator with antineoplastic, anti-inflammatory, and antiangiogenic activity. Roquinimex suppresses TH1 lymphocyte cytokines (IL-2, IFN-γ), promotes TH2 lymphocyte cytokines (IL-4, IL-10), increases NK cell, activated monocyte, and T cell activity. Roquinimex blocks macrophage TNF-α production and suppresses IL-1/IL-6 secretion. Roquinimex exhibits in vivo antitumour activity, suppresses rodent autoimmune disease signs, and ameliorates murine colitis and psoriasis. Roquinimex can be used for the research of leukemia, inflammatory bowel disease, multiple sclerosis, and psoriasis.

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

Roquinimex

Roquinimex Chemical Structure

CAS No. : 84088-42-6

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Roquinimex:

Roquinimex Related Antibodies

Top Publications Citing Use of Products

View All TNF Receptor Isoform Specific Products:

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

View All Interleukin Related Isoform Specific Products:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Roquinimex (Linomide) is an orally active immunomodulator with antineoplastic, anti-inflammatory, and antiangiogenic activity. Roquinimex suppresses TH1 lymphocyte cytokines (IL-2, IFN-γ), promotes TH2 lymphocyte cytokines (IL-4, IL-10), increases NK cell, activated monocyte, and T cell activity. Roquinimex blocks macrophage TNF-α production and suppresses IL-1/IL-6 secretion. Roquinimex exhibits in vivo antitumour activity, suppresses rodent autoimmune disease signs, and ameliorates murine colitis and psoriasis. Roquinimex can be used for the research of leukemia, inflammatory bowel disease, multiple sclerosis, and psoriasis[1][2][3][4][5].

Cellular Effect
Cell Line Type Value Description References
HUVEC IC50
13.95 μM
Compound: 1 (Linomide)
Inhibitory concentration against Human umbilical vein endothelial cell (HUVEC) proliferation
Inhibitory concentration against Human umbilical vein endothelial cell (HUVEC) proliferation
[PMID: 12643940]
PC-3 IC50
> 100 μM
Compound: 1 (Linomide)
Antiproliferative activity against PC-3 prostate cancer cells
Antiproliferative activity against PC-3 prostate cancer cells
[PMID: 12643940]
In Vitro

Roquinimex (1-100 μg/mL; 48 h) significantly reduces the number of MBP-reactive IFN-γ secreting peripheral blood MNC, but does not affect PHA-reactive IFN-γ secreting cells[3].
Roquinimex (100 μg/mL; 48 h) reduces pro-inflammatory TNF-α mRNA expression across MBP-, PPD-, and PHA-reactive peripheral blood MNC, while increasing anti-inflammatory TGF-β and IL-10 mRNA expression in MBP- and PHA-reactive cells, with no effect on IFN-γ, LT, or IL-4 mRNA expression[3].

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

Roquinimex Related Antibodies
In Vivo

Roquinimex (300 mg/kg/day; s.c.; daily; 8 days; strated from day 3 pre-DSS challenge) ameliorates dextran sodium sulfate (DDS) (HY-116282C)-induced murine colitis[2].
Roquinimex ameliorates manifestations of lupus-like disease in MRL/lpr mice[3].
Roquinimex (p.o.) provides complete protection from insulitis and maintains normal glucose tolerance for over 40 weeks in NOD mice[3].
Roquinimex (0.5-1% w/w; topical; twice daily; 8 days) exerts antipsoriatic effects in Imiquimod (HY-B0180)-induced mice[5].

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

Animal Model: Balb/c mice (male, 21-26 g) with colitis induced by 5% DDS in drinking water for 5 days[2]
Dosage: 300 mg/kg/day
Administration: s.c.; daily; 8 days; strated from day 3 pre-DSS challenge
Result: Reduced disease activity index by 60% after 5 days of DSS exposure and by 72% over the full experimental period.
Reduced mucosal damage score.
Prevented DSS-induced crypt height reduction.
Reduced colonic myeloperoxidase activity by 53%.
All outcomes were statistically significant.
Animal Model: Swiss Albino mice (male, 8-12 weeks old, 24-30 g) with psoriasis induced by Imiquimod[5]
Dosage: 0.5%; 1% w/w
Administration: topical; twice daily; 8 days
Result: Reduced mean Baker's histopathological score.
Increased skin tissue IL-10 levels.
Reduced skin tissue IL-17 levels.
Reduced skin tissue TNF-α levels.
Reduced skin tissue VEGF levels.
Improved histopathological features, including mild keratosis, no Munro's abscesses or parakeratosis, mild acanthosis, few or no rete ridges, mild papillary thinning, and mild or few dermal lymphocytic infiltrations.
Showed statistically significant improvements.
Molecular Weight

308.33

Formula

C18H16N2O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(O)C2=C(N(C)C1=O)C=CC=C2)N(C)C3=CC=CC=C3
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 : ≥ 83.3 mg/mL (270.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2433 mL 16.2164 mL 32.4328 mL
5 mM 0.6487 mL 3.2433 mL 6.4866 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.69%

SDS (479 KB)

COA (250 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2433 mL 16.2164 mL 32.4328 mL 81.0820 mL
5 mM 0.6487 mL 3.2433 mL 6.4866 mL 16.2164 mL
10 mM 0.3243 mL 1.6216 mL 3.2433 mL 8.1082 mL
15 mM 0.2162 mL 1.0811 mL 2.1622 mL 5.4055 mL
20 mM 0.1622 mL 0.8108 mL 1.6216 mL 4.0541 mL
25 mM 0.1297 mL 0.6487 mL 1.2973 mL 3.2433 mL
30 mM 0.1081 mL 0.5405 mL 1.0811 mL 2.7027 mL
40 mM 0.0811 mL 0.4054 mL 0.8108 mL 2.0270 mL
50 mM 0.0649 mL 0.3243 mL 0.6487 mL 1.6216 mL
60 mM 0.0541 mL 0.2703 mL 0.5405 mL 1.3514 mL
80 mM 0.0405 mL 0.2027 mL 0.4054 mL 1.0135 mL
100 mM 0.0324 mL 0.1622 mL 0.3243 mL 0.8108 mL
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Roquinimex 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.

Keywords:

Roquinimex84088-42-6Linomide FCF89 ABR212616FCF89FCF 89FCF-89ABR212616ABR 212616ABR-212616TNF ReceptorInterleukin RelatedIFNARTumor Necrosis Factor ReceptorTNFRILInterferon-α/β receptorInterferon-alpha/beta receptoracute myelogenous leukemiainflammatory bowel diseaseNK cellchronic myelogenous leukemiaTH1 lymphocyte cytokinesmultiple sclerosisadvanced renal cell carcinomaadvanced malignant melanomaeccrine sweat glandTH2 lymphocyte cytokinesInhibitorinhibitorinhibit

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