Cat. No.: HY-13743

Roquinimex

(Synonyms: Linomide; FCF89; ABR212616)

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Based on 1 Customer Validation

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.

Purity: 99.69%
CAS No.: 84088-42-6
Formula: C₁₈H₁₆N₂O₃
Molecular Weight:308.33

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Roquinimex Chemical Structure

CAS No.: 84088-42-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All TNF Receptor Isoforms :

All Interleukin Related Isoforms :

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.

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.

Chemical Information

CAS No. 84088-42-6
Appearance Solid
Molecular Weight 308.33
Formula C₁₈H₁₆N₂O₃
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
Synonyms

Linomide; FCF89; ABR212616
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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.2433 mL

16.2164 mL

32.4328 mL

5 mM

0.6487 mL

3.2433 mL

6.4866 mL

10 mM

0.3243 mL

1.6216 mL

3.2433 mL

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.

Molarity Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (295 KB)
SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Ohsuga Y, et al. Dermatologic changes associated with roquinimex immunotherapy after autologous bone marrow transplant. J Am Acad Dermatol. 2000;43(3):437-441. [Content Brief]

[2]. Liu Q, et al. Roquinimex inhibits dextran sodium sulfate-induced murine colitis. Inflamm Res. 2003;52(2):64-68. [Content Brief]

[3]. Tian WZ, et al. Linomide (roquinimex) affects the balance between pro- and anti-inflammatory cytokines in vitro in multiple sclerosis. Acta Neurol Scand. 1998;98(2):94-101. [Content Brief]

[4]. Mackean MJ, et al. A feasibility study of roquinimex (Linomide) and alpha interferon in patients with advanced malignant melanoma or renal carcinoma. Br J Cancer. 1998;78(12):1620-1623. [Content Brief]

[5]. Hasan AM, et al. Novel effect of topical Roquinimex and its combination with Clobetasol on an imiquimod-induced model of psoriasis in mice. Naunyn Schmiedebergs Arch Pharmacol. 2024;397(7):5219-5232. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Apoptosis Compound Library

Immunology/Inflammation Compound Library

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Mass Spectrometry Human Metabolite Library

All TNF Receptor Isoforms

All Interleukin Related Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Roquinimex Related Classifications

HY-13743 Related Classifications