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[CAS NO. 130641-38-2] Bindarit
| Ships within | Stock | Price | Qty | Total |
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| Catalog: | HY-B0498 |
| Brand: | MCE |
| CAS: | 130641-38-2 |
Overview
| MDL | MFCD00866723 |
|---|---|
| Molecular Weight | 324.37 |
| Molecular Formula | C19H20N2O3 |
| SMILES | CC(OCC1=NN(CC2=CC=CC=C2)C3=C1C=CC=C3)(C)C(O)=O |
12 Publications Citing Use of MCE
- [1]Nat Nanotechnol. 2021 Jul;16(7):830-839.
- [2]Materials Today. 2022.
- [3]Cell Death Differ. 2021 Sep;28(9):2616-2633.
- [4]Theranostics. 2021 Jan 25;11(8):3624-3641.
- [5]Adv Healthc Mater. 2022 Dec 22;e2201705.
- [6]Brain Behav Immun. 2020 Oct;89:400-413.
- [7]Cell Death Dis. 2022 Aug 29;13(8):748.
- [8]Stem Cell Res Ther. 2021 Jul 2;12(1):378.
- [9]Immunology. 2022 Jun 11.
- [10]Int J Oncol. 2022 Feb;60(2):19.
- [11]Immunopharmacol Immunotoxicol. 2021 Dec 17;1-10.
- [12]Life. 2022, 12(6), 836.
Summary
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 [1] .
IC50 & Target
MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8 [1]
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] .
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] .
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 |
|---|---|---|---|---|
| NCT01269242 | Aziende Chimiche Riunite Angelini Francesco S.p.A |
Coronary Restenosis
|
January 2009 | Phase 2 |
| NCT01109212 | Aziende Chimiche Riunite Angelini Francesco S.p.A|Mario Negri Institute for Pharmacological Research |
Diabetic Nephropathy
|
March 2007 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 46 mg/mL ( 141.81 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 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 |
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.
- [2] Zoja C, Bindarit retards renal disease and prolongs survival in murine lupus autoimmune disease. Kidney Int. 1998 Mar;53(3):726-34.
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