Bindarit

Modify Date: 2025-08-21 19:17:04

Bindarit Structure
Bindarit structure
 Common Name Bindarit
CAS Number 130641-38-2 Molecular Weight 324.374
Density 1.2±0.1 g/cm3 Boiling Point 542.9±40.0 °C at 760 mmHg
Molecular Formula C19H20N2O3 Melting Point N/A
MSDS N/A Flash Point 282.1±27.3 °C

 Use of Bindarit


Bindarit(AF-2838), a CCL2, CCL7 and CCL8 inhibitor, is an anti-inflammatory agent.Target: OthersBindarit 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].

 Names

Name 2-[(1-benzylindazol-3-yl)methoxy]-2-methylpropanoic acid
Synonym More Synonyms

 Bindarit Biological Activity

Description Bindarit(AF-2838), a CCL2, CCL7 and CCL8 inhibitor, is an anti-inflammatory agent.Target: OthersBindarit 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].
Related Catalog
References

[1]. Zoja, C., et al., Bindarit retards renal disease and prolongs survival in murine lupus autoimmune disease. Kidney Int, 1998. 53(3): p. 726-34.

[2]. Gazzaniga, S., et al., Targeting tumor-associated macrophages and inhibition of MCP-1 reduce angiogenesis and tumor growth in a human melanoma xenograft. J Invest Dermatol, 2007. 127(8): p. 2031-41.

[3]. Grassia, G., et al., The anti-inflammatory agent bindarit inhibits neointima formation in both rats and hyperlipidaemic mice. Cardiovasc Res, 2009. 84(3): p. 485-93.

[4]. Zollo, M., et al., Targeting monocyte chemotactic protein-1 synthesis with bindarit induces tumor regression in prostate and breast cancer animal models. Clin Exp Metastasis, 2012. 29(6): p. 585-601.

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 542.9±40.0 °C at 760 mmHg
Molecular Formula C19H20N2O3
Molecular Weight 324.374
Flash Point 282.1±27.3 °C
Exact Mass 324.147400
PSA 64.35000
LogP 3.44
Vapour Pressure 0.0±1.5 mmHg at 25°C
Index of Refraction 1.595
InChIKey MTHORRSSURHQPZ-UHFFFAOYSA-N
SMILES CC(C)(OCc1nn(Cc2ccccc2)c2ccccc12)C(=O)O

 Safety Information

Hazard Codes Xi
HS Code 2933990090

 Synthetic Route

1-Benzyl-3-Iodo-1H-Indazole structure

1-Benzyl-3-Iodo...

CAS#:205643-28-3

~%

Bindarit Structure

Bindarit

CAS#:130641-38-2

Literature: WO2011/15501 A1, ;
Benzyl bromide structure

Benzyl bromide

CAS#:100-39-0

~%

Bindarit Structure

Bindarit

CAS#:130641-38-2

Literature: WO2011/15501 A1, ;
3-Bromo-1H-indazole structure

3-Bromo-1H-indazole

CAS#:40598-94-5

~%

Bindarit Structure

Bindarit

CAS#:130641-38-2

Literature: WO2011/15501 A1, ;
1-BENZYL-3-HYDROXYMETHYL-1H-INDAZOLE structure

1-BENZYL-3-HYDR...

CAS#:131427-21-9

~%

Bindarit Structure

Bindarit

CAS#:130641-38-2

Literature: WO2011/15501 A1, ;
1-benzyl-1H-indazol-3-carbaldehyde structure

1-benzyl-1H-ind...

CAS#:1186509-61-4

~%

Bindarit Structure

Bindarit

CAS#:130641-38-2

Literature: WO2011/15501 A1, ;
1-Benzyl-3-bromo-1H-indazole structure

1-Benzyl-3-brom...

CAS#:29985-03-3

~%

Bindarit Structure

Bindarit

CAS#:130641-38-2

Literature: WO2011/15501 A1, ;

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

2-[(1-Benzyl-1H-indazol-3-yl)methoxy]-2-methylpropanoic acid
Bindarit (USAN/INN)
2-((1-benzyl-1H-indazol-3-yl)methoxy)-2-methylpropanoic acid
Propanoic acid, 2-methyl-2-[[1-(phenylmethyl)-1H-indazol-3-yl]methoxy]-
bindarit
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