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Bindarit (AF2838) MCP/CCL Inhibitor

Name: Bindarit (AF2838)
Brand: Selleck Chemicals
SKU: S3032
Availability: InStock
Rating: 5 (23 reviews)

Cat.No.S3032

Bindarit exhibits selective inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8.

Chemical Structure

Molecular Weight: 324.37

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.75%

99.75

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description	PMID
SK-N-MC	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
SK-N-SH	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	324.37	Formula	C₁₉H₂₀N₂O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	130641-38-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 64 mg/mL (197.3 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 64 mg/mL

Water : Insoluble

DMSO : 200 mg/mL (616.57 mM) Ultrasonicated;
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 33 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	10%DMSO 1 90%Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	6.600mg/ml (20.35mM)	Taking the 1 mL working solution as an example, add 100 μL of 66 mg/ml clear DMSO stock solution to 900 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (30.83mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (3.08mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	8.000mg/ml (24.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 160 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	Bindarit is devoid of immunosuppressive effects.
Targets/IC₅₀/Ki	MCP-1/CCL2 ^[1] MCP-3/CCL7 ^[1] MCP-2/CCL8 ^[1]
In vitro	Bindarit treatment causes a dose-dependent inhibition of the capacity of human monocytes to produce monocyte chemotactic protein-1 (MCP-1) in response to bacterial LPS or C. albicans with IC50 of 172 µM and 403 µM, respectively. The inhibition of LP-induced MCP-1 production by this compound is associated with reduced levels of MCP-1 mRNA transcripts with IC50 of 75 µM. It inhibits the production of MCP-1 by LPS-stimulated MM6 cells with IC50 of 425 μM, without affecting the release of IL-8 or IL-6. ^[2] This chemical inhibits the release of MCP-1 from IL-1 stimulated osteoblast cell line Saos-2. ^[3] It, even at the maximal concentration, does not exhibit a direct in vitro cytotoxic effect on human IIB-MEL-J melanoma or ECs, although it inhibits MCP-1 expression. ^[4] This compound (10-300 μM) reduces rat vascular smooth muscle cell (VSMC) proliferation, migration, and invasion. ^[5] It induces the downregulation of the classical NF-κB pathway. This chemical displays a specific inhibitory effect on the p65 and p65/p50 induced MCP-1 promoter activation, with no effect on other tested activated promoters, indicating that it acts on a specific subpopulation of NF-κB isoforms and selects its targets within the whole NF-κB inflammatory pathway. ^[6] It modulates cancer-cell proliferation and migration, mainly through negative regulation of TGF-β and AKT signaling. ^[7]
In vivo	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. This compound treatment completely MCP-1 up-regulation during the progression of nephritis. ^[1] Inhibition of MCP-1 with this chemical also reduces tumor growth and macrophage recruitment, rendering necrotic tumor masses in human melanoma xenografts. ^[4] This compound 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. ^[5] Administration of this chemical 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, this treatment significantly decreases the infiltration of tumor-associated macrophages and myeloid-derived suppressor cells in 4T1-Luc primary tumors. ^[7]
References	[1] https://pubmed.ncbi.nlm.nih.gov/9507220/ [2] https://pubmed.ncbi.nlm.nih.gov/10477401/ [3] https://pubmed.ncbi.nlm.nih.gov/12056513/ [4] https://pubmed.ncbi.nlm.nih.gov/17460736/ [5] https://pubmed.ncbi.nlm.nih.gov/19592568/ [6] https://pubmed.ncbi.nlm.nih.gov/22189654/ [7] https://pubmed.ncbi.nlm.nih.gov/22484917/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01269242	Completed	Coronary Restenosis	Aziende Chimiche Riunite Angelini Francesco S.p.A	January 2009	Phase 2
NCT01109212	Completed	Diabetic Nephropathy	Aziende Chimiche Riunite Angelini Francesco S.p.A\|Mario Negri Institute for Pharmacological Research	March 2007	Phase 2

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