Cat. No.: HY-B0498

Bindarit

(Synonyms: AF2838)

29 Cited Publications

Customer Review

Based on 29 publication(s) in Google Scholar

Bindarit (AF2838) is a selective inhibitor of the monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8, and no effect on other CC and CXC chemokines such as MIP-1α/CCL3, MIP-1β/CCL4, MIP-3/CCL23. Bindarit also has anti-inflammatory activity.

For research use only. We do not sell to patients.

Purity: 99.51%
CAS No.: 130641-38-2
Formula: C₁₉H₂₀N₂O₃
Molecular Weight:324.37

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Bindarit Chemical Structure

CAS No.: 130641-38-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (29)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8^[1]

All CCR Isoforms :

In Vitro

Bindarit (10-300 μM; 48 hours) at 100 μM and 300 μM significantly inhibits platelet derived growth factor-BB (PDGF-BB)-induced rat VSMCs proliferation by 27% and 42%, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

VSMC cells
Concentration:

10 μM, 30 μM, 100 μM, 300 μM
Incubation Time:

48 hours
Result:

Inhibited PDGF-BB-induced rat VSMCs proliferation.

In Vivo

Bindarit (50 mg/kg; oral administration; every day; for 4 months, 6 months, 8 months; NZB/W F1 female mice) delays the onset of proteinuria and significantly protects from renal function impairment. Bindarit completely prevents monocyte chemoattractant protein (MCP-1) up-regulation^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NZB/W F1 female mice ( two months of age)^[2]
Dosage:

50 mg/kg
Administration:

Oral administration; every day; for 4 months, 6 months, 8 months
Result:

Delayed the onset of proteinuria and significantly protected from renal function impairment.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 130641-38-2
Appearance Solid
Molecular Weight 324.37
Formula C₁₉H₂₀N₂O₃
Color White to off-white
SMILES

CC(OCC1=NN(CC2=CC=CC=C2)C3=C1C=CC=C3)(C)C(O)=O
Synonyms

AF2838
Structure Classification
- Ketones, Aldehydes, Acids
Initial Source
- Plants
- Umbelliferae
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (29)

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Journal Impact Factor

Nat Nanotechnol

Therapeutically reprogrammed nutrient signalling enhances nanoparticulate albumin bound drug uptake and efficacy in KRAS-mutant cancer. [Abstract]

2021 Jul;16(7):830-839. PMID: 33958764
Mater Today

Overcoming pancreatic cancer immune resistance by codelivery of CCR2 antagonist using a STING-activating gemcitabine-based nanocarrier. [Abstract]

2023 Jan-Feb:62:33-50. PMID: 38239407
Cell Mol Immunol

A subpopulation of CD146+ macrophages enhances antitumor immunity by activating the NLRP3 inflammasome. [Abstract]

2023 Aug;20(8):908-923. PMID: 37308559
Cancer Res

Ephrin A1 Stimulates CCL2 Secretion to Facilitate Premetastatic Niche Formation and Promote Gastric Cancer Liver Metastasis. [Abstract]

2025 Jan 15;85(2):263-276. PMID: 39412948
Theranostics

Genome-wide CRISPR/Cas9 knockout screening uncovers a novel inflammatory pathway critical for resistance to arginine-deprivation therapy. [Abstract]

2021 Jan 25;11(8):3624-3641. PMID: 33664852
Genes Dis

2026 Feb 28.
Acta Pharm Sin B

Choroid plexus CCL2‒CCR2 signaling orchestrates macrophage recruitment and cerebrospinal fluid hypersecretion in hydrocephalus. [Abstract]

2024 Oct;14(10):4544-4559. PMID: 39525574

Bindarit purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2024 Oct;14(10):4544-4559. [Abstract]

Bindarit (300 μM) significantly inhibited CCL2 expression in ChP epithelial cells stimulated with LPS at protein levels.

Bindarit purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2024 Oct;14(10):4544-4559. [Abstract]

Bindarit (300 μM) exhibited a notable inhibition of M1 markers CD86 and iNOS expression and the proinflammatory cytokines TNF-α, IL-1β, and GM-CSF in macrophages.

Bindarit purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2024 Oct;14(10):4544-4559. [Abstract]

Bindarit (30 mg/kg; i.p.; every 12 h) significantly reduced the ventriculomegaly and CSF secretion rate induced by IVH in PHH rats.
Adv Sci (Weinh)

Deciphering the Role and Mechanism of Decidual Monocyte-Derived Macrophage Infiltration in Obstetric Antiphospholipid Syndrome at Single-Cell Resolution. [Abstract]

2025 Aug 7:e03480. PMID: 40776470
Cell Death Differ

CCL2 regulation of MST1-mTOR-STAT1 signaling axis controls BCR signaling and B-cell differentiation. [Abstract]

2021 Sep;28(9):2616-2633. PMID: 33879857

Bindarit purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2021 Sep;28(9):2616-2633. [Abstract]

Bindarit (100 μM; 37 ℃; 3 h) increased the levels of pBTK in B cells from C57BL/6J mice.

Bindarit purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2021 Sep;28(9):2616-2633. [Abstract]

Bindarit (100 μM; 37 ℃; 3 h) increased the levels of pPI3K, pAKT and pS6 in splenic B cells of C57BL/6J mice.
Research (Wash D C)

Single-Cell RNA Sequencing Analysis Reveals the Role of Macrophage-Mediated CD44-AKT-CCL2 Pathways in Renal Tubule Injury during Calcium Oxalate Crystal Formation. [Abstract]

2025 May 6:8:0690. PMID: 40330661
Cell Death Dis

Regulation of CCL2 by EZH2 affects tumor-associated macrophages polarization and infiltration in breast cancer. [Abstract]

2022 Aug 29;13(8):748. PMID: 36038549
J Exp Med

Tet2 deficiency-induced expansion of monocyte-derived macrophages promotes liver fibrosis. [Abstract]

2026 Feb 2;223(2):e20251114. PMID: 41474968
Adv Healthc Mater

Two-Dimensional Mg2 Si Nanosheet-Enabled Sustained Hydrogen Generation for Improved Repair and Regeneration of Deeply-Burned Skin. [Abstract]

2023 Apr;12(10):e2201705. PMID: 36546774
Stem Cell Res Ther

Mesenchymal stem cells alleviate idiopathic pneumonia syndrome by facilitating M2 polarization via CCL2/CCR2 axis and further inducing formation of regulatory CCR2 + CD4 + T cells. [Abstract]

2025 Mar 1;16(1):108. PMID: 40025564
Stem Cell Res Ther

Mesenchymal stem cells alleviate idiopathic pneumonia syndrome by modulating T cell function through CCR2-CCL2 axis. [Abstract]

2021 Jul 2;12(1):378. PMID: 34215321
Cell Rep

Identification of endometrial CD169+ macrophages essential for Treg cell accumulation and implantation. [Abstract]

2026 Feb 18;45(3):117040. PMID: 41712382
Brain Behav Immun

Suppression of microglial activation and monocyte infiltration ameliorates cerebellar hemorrhage induced-brain injury and ataxia. [Abstract]

2020 Oct:89:400-413. PMID: 32717406
Int J Oncol

Epigallocatechin‑3‑gallate hinders metabolic coupling to suppress colorectal cancer malignancy through targeting aerobic glycolysis in cancer‑associated fibroblasts. [Abstract]

2022 Feb;60(2):19. PMID: 35029285
Int J Mol Sci

Jurkat T-Cell Antigen-Independent Elimination of PMA-Activated Neuroblastoma Cells Is Triggered by CCL2/CCR2, Depends Upon Lipid Raft LFA1/ICAM1 Immune Synapses, Is Mediated by m-TRAIL and Is Augmented by the TrkAIII Oncoprotein. [Abstract]

2026 Feb 18;27(4):1970. PMID: 41752106
J Pathol

Lactate-mediated activation of GPR81 regulates BCR/Abl protein expression in chronic myeloid leukemia cells selected under low oxygen tension. [Abstract]

2025 Oct 23. PMID: 41128634
Immunology

Peritoneal GATA6+ macrophage drives hepatic immunopathogenesis and maintains the Treg cell niche in the liver. [Abstract]

2022 Sep;167(1):77-93. PMID: 35689656
Toxicology

Macrophage-epithelial cells crosstalk and the role of CCL2-CCR2 axis in single-walled carbon nanotubes-induced lung inflammation and fibrosis. [Abstract]

2025 Dec 27:521:154388. PMID: 41461321
Med Oncol

Salvia miltiorrhiza Bunge aqueous extract inhibits lung metastasis of breast cancer by inhibiting recruitment of M2-like macrophages via CCL2-STAT3 axis. [Abstract]

2025 Jun 27;42(8):286. PMID: 40571856
Brain Res Bull

Bindarit attenuates neuroinflammation after subarachnoid hemorrhage by regulating the CCL2/CCR2/NF-κB pathway. [Abstract]

2025 Jan:220:111183. PMID: 39743001
Life

Monocyte Chemotactic Proteins Mediate the Effects of Hyperglycemia in Chondrocytes: In Vitro Studies. [Abstract]

2022 Jun 3;12(6):836. PMID: 35743867
Immunopharmacol Immunotoxicol

Immunomodulatory effects of Inonotus obliquus polysaccharide on splenic lymphocytes infected with Toxoplasma gondii via NF-κB and MAPKs pathways. [Abstract]

2022 Feb;44(1):129-138. PMID: 34918603
bioRxiv

Characterizing the SASP-Dependent Paracrine Spreading of Senescence Between Human Brain Cell Types. [Abstract]

2026 Feb 12:2026.02.10.705129. PMID: 41726875
bioRxiv

2025 Oct 13.
Patent

US20240325565A1.

Solvent & Solubility

In Vitro:

DMSO : ≥ 46 mg/mL (141.81 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0829 mL

15.4145 mL

30.8290 mL

5 mM

0.6166 mL

3.0829 mL

6.1658 mL

10 mM

0.3083 mL

1.5414 mL

3.0829 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.67 mg/mL (8.23 mM); Clear solution

This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.67 mg/mL (8.23 mM); Clear solution

This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.67 mg/mL (8.23 mM); Clear solution; Need warming

This protocol yields a clear solution of 2.67 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 5 mg/mL (15.41 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. 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. [Content Brief]

[2]. Zoja C, Bindarit retards renal disease and prolongs survival in murine lupus autoimmune disease. Kidney Int. 1998 Mar;53(3):726-34. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.0829 mL	15.4145 mL	30.8290 mL	77.0725 mL
	5 mM	0.6166 mL	3.0829 mL	6.1658 mL	15.4145 mL
	10 mM	0.3083 mL	1.5414 mL	3.0829 mL	7.7072 mL
	15 mM	0.2055 mL	1.0276 mL	2.0553 mL	5.1382 mL
	20 mM	0.1541 mL	0.7707 mL	1.5414 mL	3.8536 mL
	25 mM	0.1233 mL	0.6166 mL	1.2332 mL	3.0829 mL
	30 mM	0.1028 mL	0.5138 mL	1.0276 mL	2.5691 mL
	40 mM	0.0771 mL	0.3854 mL	0.7707 mL	1.9268 mL
	50 mM	0.0617 mL	0.3083 mL	0.6166 mL	1.5414 mL
	60 mM	0.0514 mL	0.2569 mL	0.5138 mL	1.2845 mL
	80 mM	0.0385 mL	0.1927 mL	0.3854 mL	0.9634 mL
	100 mM	0.0308 mL	0.1541 mL	0.3083 mL	0.7707 mL

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Bindarit

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Publications Citing Use of MedChemExpress (MCE) Bindarit

All CCR Isoforms

Biological Activity

Chemical Information

Publications (29)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Bindarit Related Classifications

HY-B0498 Related Classifications