Bindarit
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.51%
- No. CAS: 130641-38-2
- Fòrmula: C19H20N2O3
- Peso molecular:324.37
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Bindarit
More- Nat Nanotechnol. 2021 Jul;16(7):830-839. [Abstract]
- Mater Today. 2023 Jan-Feb:62:33-50. [Abstract]
- Cell Mol Immunol. 2023 Aug;20(8):908-923. [Abstract]
- Cancer Res. 2025 Jan 15;85(2):263-276. [Abstract]
- Theranostics. 2021 Jan 25;11(8):3624-3641. [Abstract]
- Genes Dis. 2026 Feb 28.
- Acta Pharm Sin B. 2024 Oct;14(10):4544-4559. [Abstract]
- Adv Sci (Weinh). 2025 Aug 7:e03480. [Abstract]
- Cell Death Differ. 2021 Sep;28(9):2616-2633. [Abstract]
- Research (Wash D C). 2025 May 6:8:0690. [Abstract]
- Cell Death Dis. 2022 Aug 29;13(8):748. [Abstract]
- J Exp Med. 2026 Feb 2;223(2):e20251114. [Abstract]
- Adv Healthc Mater. 2023 Apr;12(10):e2201705. [Abstract]
- Stem Cell Res Ther. 2025 Mar 1;16(1):108. [Abstract]
- Stem Cell Res Ther. 2021 Jul 2;12(1):378. [Abstract]
- Cell Rep. 2026 Feb 18;45(3):117040. [Abstract]
- Brain Behav Immun. 2020 Oct:89:400-413. [Abstract]
- Int J Oncol. 2022 Feb;60(2):19. [Abstract]
- Int J Mol Sci. 2026 Feb 18;27(4):1970. [Abstract]
- J Pathol. 2025 Oct 23. [Abstract]
- Immunology. 2022 Sep;167(1):77-93. [Abstract]
- Toxicology. 2025 Dec 27:521:154388. [Abstract]
- Med Oncol. 2025 Jun 27;42(8):286. [Abstract]
- Brain Res Bull. 2025 Jan:220:111183. [Abstract]
- Life. 2022 Jun 3;12(6):836. [Abstract]
- Immunopharmacol Immunotoxicol. 2022 Feb;44(1):129-138. [Abstract]
- bioRxiv. 2026 Feb 12:2026.02.10.705129. [Abstract]
- bioRxiv. 2025 Oct 13.
- Patent. US20240325565A1.
Customer Validation & Images
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Histological Imaging/Staining
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Actividad biológica
MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8[1]
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.
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Cell Line:VSMC cells
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Concentration:10 μM, 30 μM, 100 μM, 300 μM
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Incubation Time:48 hours
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Result:Inhibited PDGF-BB-induced rat VSMCs proliferation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NZB/W F1 female mice ( two months of age)[2]
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Dosage:50 mg/kg
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Administration:Oral administration; every day; for 4 months, 6 months, 8 months
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Result:Delayed the onset of proteinuria and significantly protected from renal function impairment.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 130641-38-2
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Appearance Solid
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Peso molecular 324.37
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Fòrmula C19H20N2O3
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Color White to off-white
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SMILES
CC(OCC1=NN(CC2=CC=CC=C2)C3=C1C=CC=C3)(C)C(O)=O
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Synonyms
AF2838
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Structure Classification
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Initial Source
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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
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Most Recent
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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 -
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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.
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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.
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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 -
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Solvente y solubilidad
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 5 mg/mL (15.41 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (281 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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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