Bindarit (Synonyms: AF 2838) |
Catalog No.GC13335
One-Click Copy Product Info
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Bindarit is an indazolic derivative that exhibits anti-inflammatory activity in different models.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 130641-38-2
Sample solution is provided at 25 µL, 10mM.
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Bindarit is an indazolic derivative that exhibits anti-inflammatory activity in different models[1]. Bindarit specifically inhibits p65- and p65/p50-mediated activation of the MCP-1 promoter, and directly interacts with FABP4 by increasing expression and nuclear localization, thereby affecting peroxisome proliferator-activated receptor γ (PPARγ) and lipopolysaccharide (LPS) -dependent kinase signaling pathways[2]. Bindarit has been widely used to prevent bone loss caused by Chikungunya virus infection[3].
In vitro, Bindarit treatment (100µM) for 48 hours significantly inhibited the proliferation and migration of coronary artery smooth muscle cells (CASMCs) induced by TNF-α (30ng/ml)[4]. Pretreatment with 300µM Bindarit for 1 hour significantly reduced Angiotensin II, endothelin-1, and TGFβ-induced contraction of human renal mesangial cells (HRMCs) and phosphorylation of vinculin protein[5].
In vivo, Bindarit treatment via oral administration at a dose of 100mg/kg twice daily for 10 days significantly alleviated trinitro-benzene sulfonic acid (TNBS)-induced colitis in mice, reduced leukocyte infiltration, and downregulated MCP-1 synthesis[6]. Daily intraperitoneal injection of Bindarit at a dose of 100mg/kg for 12 weeks significantly inhibited tumor growth and metastasis in the PC-3M-Luc2 xenograft mouse model, and improved survival rate[7]. Subcutaneous injection of Bindarit at a dose of 100mg/kg daily for 28 days alleviated brain injury, maintained blood-brain barrier integrity, and mitigated neuroinflammation in mice with status epilepticus[8].
References:
[1] Grassia G, Maddaluno M, Guglielmotti A, et al. The anti-inflammatory agent bindarit inhibits neointima formation in both rats and hyperlipidaemic mice[J]. Cardiovascular research, 2009, 84(3): 485-493.
[2] Oddi S, Scipioni L, Totaro A, et al. The anti-inflammatory agent bindarit acts as a modulator of fatty acid-binding protein 4 in human monocytic cells[J]. Scientific reports, 2019, 9(1): 15155.
[3] Chen W, Foo S S, Taylor A, et al. Bindarit, an inhibitor of monocyte chemotactic protein synthesis, protects against bone loss induced by chikungunya virus infection[J]. Journal of virology, 2015, 89(1): 581-593.
[4] Maddaluno M, Grassia G, Di Lauro M V, et al. Bindarit inhibits human coronary artery smooth muscle cell proliferation, migration and phenotypic switching[J]. Plos one, 2012, 7(10): e47464.
[5] Paccosi S, Giachi M, Di Gennaro P, et al. The chemokine (CC motif) ligand protein synthesis inhibitor bindarit prevents cytoskeletal rearrangement and contraction of human mesangial cells[J]. Cytokine, 2016, 85: 92-100.
[6] Bhatia M, Landolfi C, Basta F, et al. Treatment with bindarit, an inhibitor of MCP-1 synthesis, protects mice against trinitrobenzene sulfonic acid-induced colitis[J]. Inflammation research, 2008, 57(10): 464-471.
[7] Zollo M, Di Dato V, Spano D, et al. Targeting monocyte chemotactic protein-1 synthesis with bindarit induces tumor regression in prostate and breast cancer animal models[J]. Clinical & experimental metastasis, 2012, 29(6): 585-601.
[8] Chen J, Hu Y, Xie J, et al. Bindarit attenuates brain injury and neuroinflammation in status epilepticus by disrupting C3/C3aR signaling and modulating microglia-astrocyte interactions[J]. Cell Communication and Signaling, 2026.
| Cell experiment [1]: | |
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Cell lines |
Human coronary artery smooth muscle cells (CASMCs) |
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Preparation Method |
CASMCs were cultured in smooth muscle basal medium supplemented with 0.5mg/ml hEGF, 5mg/ml insulin, 1mg/ml hFGF, 50mg/ml gentamicin/amphotericin-B, 5% fetal bovine serum (FBS) at 37°C in 5% CO2/atmosphere. Cells cultured were seeded onto 24-well microplates (1.5×104 cells/well) and cultured for 24h. After the induction of quiescence, cells were stimulated with TNF-α (30ng/ml) or FBS (5%) for 48 hours in the presence or absence of Bindarit (10, 25, 50, 100, 200, and 300µM), and cell proliferation was assessed. |
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Reaction Conditions |
10, 25, 50, 100, 200, and 300µM; 48h |
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Applications |
Bindarit treatment reduced the cell proliferation of CASMCs induced by TNF-α in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Female BALB/c mice |
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Preparation Method |
Female BALB/c mice (6 weeks old) were housed under controlled temperature (21-23°C), humidity (30-35%), and light cycle (7:00 AM to 7:00 PM) and maintained on a standard rodent diet. 2.5×105 4T1-Luc cells per 100μl PBS were orthotopically transplanted into the mammary fat pads of 10-week-old BALB/c mice. 100mg/kg Bindarit was administered by oral gavage, once a day, for five consecutive days per week, for 2 weeks. Tumor growth was monitored by bioluminescent (BLI). |
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Dosage form |
100mg/kg; five times a week, 2 weeks; p.o. |
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Applications |
Bindarit treatment significantly inhibited local tumorigenesis and tumor growth in mice with 4T1-Luc xenografts. |
References: [1] Maddaluno M, Grassia G, Di Lauro M V, et al. Bindarit inhibits human coronary artery smooth muscle cell proliferation, migration and phenotypic switching[J]. Plos one, 2012, 7(10): e47464. [2] Zollo M, Di Dato V, Spano D, et al. Targeting monocyte chemotactic protein-1 synthesis with bindarit induces tumor regression in prostate and breast cancer animal models[J]. Clinical & experimental metastasis, 2012, 29(6): 585-601. | |
| Cas No. | 130641-38-2 | SDF | |
| Synonyms | AF 2838 | ||
| Chemical Name | 2-[(1-benzylindazol-3-yl)methoxy]-2-methylpropanoic acid | ||
| Canonical SMILES | CC(C)(C(=O)O)OCC1=NN(C2=CC=CC=C21)CC3=CC=CC=C3 | ||
| Formula | C19H20N2O3 | M.Wt | 324.37 |
| Solubility | ≥ 16.2mg/mL in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0829 mL | 15.4145 mL | 30.829 mL |
| 5 mM | 616.6 μL | 3.0829 mL | 6.1658 mL |
| 10 mM | 308.3 μL | 1.5414 mL | 3.0829 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)