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Chemical Structure| 248282-01-1 Chemical Structure| 248282-01-1

Structure of Paquinimod
CAS No.: 248282-01-1

Chemical Structure| 248282-01-1

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Paquinimod is an inhibitor of S100A9 which can prevent S100A9 from binding to TLR-4. Paquinimod is also known as ABR‑215757.

Synonyms: ABR 25757; ABR-215757

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Product Details of Paquinimod

CAS No. :248282-01-1
Formula : C21H22N2O3
M.W : 350.41
SMILES Code : O=C(C1=C(O)C2=C(N(C)C1=O)C=CC=C2CC)N(CC)C3=CC=CC=C3
Synonyms :
ABR 25757; ABR-215757
MDL No. :MFCD18633277
InChI Key :DIKSYHCCYVYKRO-UHFFFAOYSA-N
Pubchem ID :54684617

Safety of Paquinimod

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Mouse renal tubular epithelial cells (mRTECs) 150 µM 2 hours To verify the effect of Paquinimod on LPS-induced oxidative stress, apoptosis, and mitochondrial fission-fusion balance. Results showed that Paquinimod significantly inhibited LPS-induced oxidative stress and apoptosis and improved mitochondrial fission-fusion balance. Front Pharmacol. 2023 Jul 20;14:1172356
Mouse monocyte/macrophage cell line (RAW264.7) 150 µM 2 hours To verify the effect of Paquinimod on LPS-induced oxidative stress, apoptosis, and mitochondrial fission-fusion balance. Results showed that Paquinimod significantly inhibited LPS-induced oxidative stress and apoptosis and improved mitochondrial fission-fusion balance. Front Pharmacol. 2023 Jul 20;14:1172356
AGS cells 0.5 µM 24 hours Verify the inhibitory effect of Paquinimod on the proliferation and migration of AGS cells Sci Rep. 2024 Oct 9;14(1):23574
Ly6Chigh bone marrow monocytes 10 or 30 µg/ml 24 hours To investigate the effect of Paquinimod on the migratory capacity of Ly6Chigh monocytes. Results showed that Paquinimod significantly inhibited S100A9 and CT26 tumor supernatant-induced migration of Ly6Chigh monocytes. Front Immunol. 2024 Oct 21;15:1479502
Bone marrow-derived macrophages (BMDMs) 12.5–930 µg/mL 24 hours To evaluate the effect of Paquinimod on TNF release from C. albicans-infected BMDMs, results showed that Paquinimod significantly reduced TNF release Front Immunol. 2021 Feb 26;12:553911
HSG cells 300 µM 30 minutes To evaluate the effect of Paquinimod on Ca2+ signaling, results showed that Paquinimod treatment increased Ca2+ influx Clin Transl Med. 2023 Apr;13(4):e1228
Platelets 1 μg/ml 4 hours To evaluate S100A8/A9-induced platelet pyroptosis and the inhibitory effect of Paquinimod Nat Cardiovasc Res. 2022;1(8):732-747

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD mice Non-obese diabetic (NOD) mouse model Oral (via drinking water) 0.04, 0.2, 1, and 5 mg/kg/day Treatment started at 10 or 15 weeks of age and lasted for 5 to 23 weeks To evaluate the preventive efficacy of Paquinimod on diabetes development in NOD mice. Results showed that Paquinimod treatment significantly reduced the incidence of diabetes and delayed disease onset in a dose-dependent manner. Additionally, treatment significantly reduced insulitis, correlating with a selective reduction in the number of splenic macrophages and inflammatory monocytes. PLoS One. 2018 May 9;13(5):e0196598
Mice Aged mice Oral 1 mg/kg/day Three times a week for 4 weeks Paquinimod reduced the infiltration of S100A8+ T cells and myeloid cells in BAT, restored sympathetic innervation and thermogenic function, and delayed the aging process of BAT. Nat Commun. 2023 Jun 2;14(1):3208
BALB/c mice CT26 colon carcinoma model Intraperitoneal injection 1 mg/mL Daily from day 0 to day 11 To investigate the effect of Paquinimod on tumor growth and anti-PD-L1 therapy efficacy. Results showed that Paquinimod treatment increased tumor growth and reduced the efficacy of anti-PD-L1 therapy. Additionally, Paquinimod reduced the infiltration of Ly6Chigh monocytes in tumors. Front Immunol. 2024 Oct 21;15:1479502
C57BL/6 mice Bleomycin-induced pulmonary fibrosis model Intraperitoneal injection 1.0 mg/kg Daily administration until the end of the experiment Paquinimod treatment ameliorated fibrotic pathological changes and significantly reduced hydroxyproline content in the lung tissues of mice with bleomycin-induced pulmonary fibrosis. Additionally, paquinimod reduced the number of lymphocytes and neutrophils in BALF and suppressed endothelial–mesenchymal transition in vivo. BMJ Open Respir Res. 2024 Feb 20;11(1):e001803
C57BL/6J wild-type mice Cecal ligation and puncture (CLP)-induced sepsis model Intraperitoneal injection 10 mg/kg Once 1 day before and once 1 day after surgery To evaluate the protective effect of Paquinimod on sepsis-induced acute kidney injury. Results showed that Paquinimod significantly improved CLP-induced renal dysfunction, pathological changes, apoptosis, inflammation, and oxidative stress. Front Pharmacol. 2023 Jul 20;14:1172356
C57BL/6 mice Pneumococcal meningitis mouse model Intraperitoneal injection 10 mg/kg Once per day for 48 hours To evaluate the efficacy of Paquinimod as an adjunctive treatment in pneumococcal meningitis, showing reduced mortality and improved clinical scores J Neuroinflammation. 2017 Nov 2;14(1):214
BALB/c mice Chronic unpredictable mild stress (CUMS) model Intraperitoneal injection 10 mg/kg Once daily for 4 weeks To evaluate the effect of ABR-215757 on CUMS-induced depressive-like behaviors and neuroinflammation. Results showed that ABR-215757 alleviated CUMS-induced depressive-like behaviors and TLR4/NF-κB signaling activation. J Neuroinflammation. 2018 Sep 4;15(1):252
Mice Sepsis model Oral gavage 10 mg/kg/day Once daily for 3 days To evaluate the impact of Paquinimod on sepsis-induced immunosuppression, results showed that Paquinimod could partially reverse sepsis-induced immunosuppression. Mil Med Res. 2023 Jun 19;10(1):27
Mice (C57BL/6) Streptozotocin (STZ)-induced diabetic model Oral (via drinking water) 10 mg/kg/day Daily administration for 4 weeks To evaluate the effect of Paquinimod on thrombopoiesis and atherosclerosis in diabetic mice. Results showed Paquinimod significantly reduced reticulated platelets, Kupffer cell IL-6 expression, BM MkPs, and attenuated atherosclerosis progression. J Clin Invest. 2017 Jun 1;127(6):2133-2147
Mice CLP-induced sepsis model Oral gavage 10 mg/kg/day Once daily for 5 days To evaluate the effect of Paquinimod on inflammatory response and survival rate in septic mice Nat Cardiovasc Res. 2022;1(8):732-747
Mice DSS-induced acute colitis model Oral (via drinking water) 10 mg/kg/day Once daily for 14 days (7 days before DSS treatment and during 7 days of DSS treatment) To evaluate the prophylactic effect of Paquinimod on DSS-induced colitis and neuroinflammation. Results showed that Paquinimod attenuated colitis severity and systemic and neuroinflammation, reducing inflammatory markers in the colon and brain. J Neuroinflammation. 2021 Nov 10;18(1):263
Mice DSS-induced colitis model Intraperitoneal injection 10 mg/kg/day Once daily for 10 days Inhibits S100A9 activity, alleviates colitis symptoms Cell Mol Gastroenterol Hepatol. 2025;19(6):101486
Mice NASH model induced by high-fat diet plus adenovirus-CXCL1 overexpression Intraperitoneal injection 10 or 20 mg/kg Every second day for two weeks To evaluate the therapeutic effect of Paquinimod on NASH phenotype, results showed that Paquinimod significantly reduced serum ALT and AST levels, decreased adipose tissue lipolysis and inflammation, and ameliorated the NASH phenotype. Cell Mol Gastroenterol Hepatol. 2022;13(1):151-171
Mice SARS-CoV-2 infection model Intranasal administration 12.5 mg/day Daily administration starting from day 2 post-infection Paquinimod significantly reduced lung damage and viral loads in SARS-CoV-2-infected mice and improved their survival status. Cell Host Microbe. 2021 Feb 10;29(2):222-235. e4
Nonobese diabetic (NOD) mice Sjögren’s dry eye disease (SjDED) model Intraperitoneal injection 25 mg/kg Every other day for 4 weeks To evaluate the effect of paquinimod on dry eye disease, results showed that paquinimod ameliorated clinical and histopathological phenotypes of SjDED mice and reduced the proportion of Th17 cells in LGs, lymph nodes, and spleens. Invest Ophthalmol Vis Sci. 2025 Jan 2;66(1):35
Mice TAC surgery model Ad libitum in drinking water 3.75 mg/kg Continued for four weeks Inhibited S100A8/9, alleviated ponatinib-induced cardiac dysfunction Circ Res. 2023 Feb 3;132(3):267-289
Mice (C57BL/6) Intra-abdominal candidiasis (IAC) model Intraperitoneal injection 30 mg/kg Every 24 hours until the end of the experiment To evaluate the effect of Paquinimod on inflammatory collateral tissue damage (ICTD) in the IAC model, results showed that Paquinimod significantly reduced ICTD and improved survival Front Immunol. 2021 Feb 26;12:553911
Mice Traumatic brain injury (TBI) model Intraperitoneal injection 4, 10, and 25 mg/kg/day Once daily for three consecutive days To evaluate the effect of Paquinimod on neuroinflammation and neurological function after traumatic brain injury. Results showed that Paquinimod significantly alleviated neuroinflammation and neuronal death, improving neurological function. Redox Biol. 2025 Apr;81:103532
Sprague-Dawley (SD) rats Acute myocardial infarction model Intraperitoneal injection 5 mg/kg/day Once daily for 5 consecutive days To evaluate the effect of Paquinimod on improving depression-like behavior and cardiac function after acute myocardial infarction, results showed that Paquinimod significantly improved cardiac function and reduced depression-like behavior. Front Pharmacol. 2022 Jun 24;13:832590
Mice IL14 α transgenic mice Oral 5 mg/kg/day Once daily for 9 weeks To evaluate the effect of Paquinimod on the phenotype of IL14 α transgenic mice, results showed that Paquinimod treatment reduced immune cell infiltration and restored salivary gland function Clin Transl Med. 2023 Apr;13(4):e1228
Mice CLP-induced sepsis model Intraperitoneal injection 5-20 mg/kg Before and after CLP operation Paquinimod significantly reduced CLP-induced liver dysfunction and injury, and improved mitochondrial function Int J Mol Sci. 2023 Jan 20;24(3):2112
Lewis rats Experimental Autoimmune Uveitis (EAU) Oral Approximately 25 mg/kg/day Daily, throughout the experiment To evaluate the effect of Paquinimod on EAU recurrence. Results showed that Paquinimod significantly protected tEAU rats from recurrence, reduced the number of Th1 and Th17 cells, and increased the number of Tregs. Invest Ophthalmol Vis Sci. 2018 Mar 1;59(3):1332-1342

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01487551 Systemic Sclerosis Phase 2 Completed - Germany ... More >> Berlin, Germany Cologne, Germany Erlangen, Germany Sweden Gothenburg, Sweden Lund, Sweden Switzerland Zürich, Switzerland Less <<
NCT00997100 Systemic Lupus Erythematosus Phase 2 Completed - Denmark ... More >> Soren Jacobsen Copenhagen, Denmark, 2100 Sweden Dept of Rheumatology, University Hospital in Lund Lund, Sweden, 220 07 Iva Gunnarsson M.D. Stockholm, Sweden, 171 76 Lars Rönnblom M.D. Uppsala, Sweden, 751 85 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.85mL

0.57mL

0.29mL

14.27mL

2.85mL

1.43mL

28.54mL

5.71mL

2.85mL

References

 

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