BindaritCAS# 130641-38-2 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 130641-38-2 | SDF | Download SDF |
| PubChem ID | 71354 | Appearance | Powder |
| Formula | C19H20N2O3 | M.Wt | 324.37 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | AF2838 | ||
| Solubility | DMSO : ≥ 46 mg/mL (141.81 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 2-[(1-benzylindazol-3-yl)methoxy]-2-methylpropanoic acid | ||
| SMILES | CC(C)(C(=O)O)OCC1=NN(C2=CC=CC=C21)CC3=CC=CC=C3 | ||
| Standard InChIKey | MTHORRSSURHQPZ-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C19H20N2O3/c1-19(2,18(22)23)24-13-16-15-10-6-7-11-17(15)21(20-16)12-14-8-4-3-5-9-14/h3-11H,12-13H2,1-2H3,(H,22,23) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Bindarit(AF-2838), a CCL2, CCL7 and CCL8 inhibitor, is an anti-inflammatory agent.
Target: Others
Bindarit exhibits selective inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8. Oral administration of Bindarit at 50 mg/kg in NZB/W mice delays the onset of proteinuria, significantly protects from renal function impairment, and prolongs survival of NZB/W mice or lupus mice. Bindarit treatment completely MCP-1 up-regulation during the progression of nephritis [1]. Inhibition of MCP-1 with Bindarit also reduces tumor growth and macrophage recruitment, rendering necrotic tumor masses in human melanoma xenografts [2]. Bindarit is effective in reducing neointima formation in both non-hyperlipidaemic and hyperlipidaemic animal models of vascular injury by a direct effect on VSMC proliferation and migration and by reducing neointimal macrophage content [3]. Administration of Bindarit results in impaired metastatic disease in prostate cancer PC-3M-Luc2 xenograft mice and impairment of local tumorigenesis in Balb/c mice with murine breast cancer 4T1-Luc cells. In addition, Bindarit treatment significantly decreases the infiltration of tumor-associated macrophages and myeloid-derived suppressor cells in 4T1-Luc primary tumors [4]. References: | |||||
Bindarit Dilution Calculator
Bindarit Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.0829 mL | 15.4145 mL | 30.829 mL | 61.658 mL | 77.0725 mL |
| 5 mM | 0.6166 mL | 3.0829 mL | 6.1658 mL | 12.3316 mL | 15.4145 mL |
| 10 mM | 0.3083 mL | 1.5414 mL | 3.0829 mL | 6.1658 mL | 7.7072 mL |
| 50 mM | 0.0617 mL | 0.3083 mL | 0.6166 mL | 1.2332 mL | 1.5414 mL |
| 100 mM | 0.0308 mL | 0.1541 mL | 0.3083 mL | 0.6166 mL | 0.7707 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Bindarit exhibits selective inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8.
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The chemokine (C-C motif) ligand protein synthesis inhibitor bindarit prevents cytoskeletal rearrangement and contraction of human mesangial cells.[Pubmed:27309675]
Cytokine. 2016 Sep;85:92-100.
Intraglomerular mesangial cells (MCs) maintain structural and functional integrity of renal glomerular microcirculation and homeostasis of mesangial matrix. Following different types of injury, MCs change their phenotype upregulating the expression of alpha-smooth muscle actin (alpha-SMA), changing contractile abilities and increasing the production of matrix proteins, chemokines and cytokines. CCL2 is a chemokine known to be involved in the pathogenesis of renal diseases. Its glomerular upregulation correlates with the extent of renal damage. Bindarit is an indazolic derivative endowed with anti-inflammatory activity when tested in experimental diseases. It selectively inhibits the synthesis of inflammatory C-C chemokines including CCL2, CCL7 and CCL8. This work aims to analyse Bindarit effects on ET1-, AngII- and TGFbeta-induced mesangial cell dysfunction. Bindarit significantly reduced AngII-, ET1- and TGFbeta-induced alpha-SMA upregulation. In a collagen contraction assay, Bindarit reduced AngII-, ET1- and TGFbeta-induced HRMC contraction. Within 3-6h stimulation, vinculin organization and phosphorylation was significantly impaired by Bindarit in AngII-, ET1- and TGFbeta-stimulated cells without any effect on F-actin distribution. Conversely, p38 phosphorylation was not significantly inhibited by Bindarit. Our data strengthen the importance of CCL2 on ET-1, AngII- and TGFbeta-induced mesangial cell dysfunction, adding new insights into the cellular mechanisms responsible of Bindarit protective effects in human MC dysfunction.
Effects of MCP-1 inhibition by bindarit therapy in a rat model of polycystic kidney disease.[Pubmed:25531096]
Nephron. 2015;129(1):52-61.
BACKGROUND/AIMS: Experimental and clinical evidence suggested that monocyte chemoattractant protein-1 (MCP-1/CCL2) has a role in the development of interstitial inflammation and renal failure in polycystic kidney disease (PKD). We investigated whether Bindarit, an inhibitor of MCP-1/CCL2 synthesis, could influence the evolution of PKD in PCK rats. METHODS: PCK rats were treated from 5 to 15 weeks of age with vehicle or Bindarit. Sprague-Dawley rats served as control. For in vitro studies, murine podocytes were exposed to albumin with or without Bindarit. RESULTS: MCP-1 mRNA was upregulated in the kidney of PCK rats and reduced by Bindarit. Treatment limited overexpression of MCP-1 protein by epithelial cells of dilated tubules and cysts, and interstitial inflammatory cells. Excessive renal accumulation of monocytes/macrophages was lowered by Bindarit by 41%. Serum creatinine slightly increased in PCK rats on vehicle and was similar to controls after Bindarit. Kidney and liver cysts were not affected by treatment. Bindarit significantly reduced progressive proteinuria of PCK rats. The antiproteinuric effect was associated with the restoration of the defective nephrin expression in podocytes of PCK rats. Bindarit limited podocyte foot process effacement and ameliorated slit diaphragm frequency. In cultured podocytes, Bindarit reduced MCP-1 production in response to albumin and inhibited albumin-induced cytoskeletal remodeling and cell migration. CONCLUSION: This study showed that although Bindarit did not prevent renal cyst growth, it limited interstitial inflammation and renal dysfunction and reduced proteinuria in PKD. Thus, Bindarit could be considered a therapeutic intervention complementary to therapies specifically acting to block renal cyst growth.
A double-blind randomised study to evaluate the efficacy and safety of bindarit in preventing coronary stent restenosis.[Pubmed:26690313]
EuroIntervention. 2016 Dec 10;12(11):e1385-e1394.
AIMS: Bindarit (BND) is a selective inhibitor of monocyte chemotactic protein-1 (MCP-1/CCL2), which plays an important role in generating intimal hyperplasia. Our aim was to explore the efficacy and safety of Bindarit in preventing restenosis following percutaneous coronary intervention. METHODS AND RESULTS: A phase II, double-blind, multicentre randomised trial included 148 patients randomised into three arms (BND 600 mg, n=48; BND 1,200 mg, n=49; PLB, n=51). Bindarit was given following PCI and continued for 180 days. Monthly clinical follow-up and six-month coronary angiography were conducted. The primary endpoint was in-segment late loss; the main secondary endpoints were in-stent late loss and major adverse cardiovascular events. Efficacy analysis was carried out on two populations, ITT and PP. There were no significant differences in the baseline characteristics among the three treatment groups. In-segment and in-stent late loss at six months in BND 600, BND 1,200 and PLB were: (ITT 0.54 vs. 0.52 vs. 0.72; p=0.21), (PP 0.46 vs. 0.53 vs. 0.72; p=0.12) and (ITT 0.74 vs. 0.74 vs. 1.05; p=0.01), (PP 0.66 vs. 0.73 vs. 1.06; p=0.003), respectively. The MACE rates at nine months among treatment groups were 20.8% vs. 28.6% vs. 25.5% (p=0.54), respectively. CONCLUSIONS: This was a negative study with the primary endpoint not being met. However, significant reduction in the in-stent late loss suggests that Bindarit probably exerts a favourable action on the vessel wall following angioplasty. Bindarit was well tolerated with a compliance rate of over 90%. A larger study utilising a loading dose and targeting a specific patient cohort may demonstrate more significant results.
