1. GPCR/G Protein
    Immunology/Inflammation
  2. CCR
  3. Bindarit

Bindarit (Synonyms: AF2838)

Cat. No.: HY-B0498 Purity: 99.83%
Handling Instructions

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.

Bindarit Chemical Structure

Bindarit Chemical Structure

CAS No. : 130641-38-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 264 In-stock
Estimated Time of Arrival: December 31
10 mg USD 240 In-stock
Estimated Time of Arrival: December 31
50 mg USD 720 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
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Description

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].

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].

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
Molecular Weight

324.37

Formula

C₁₉H₂₀N₂O₃

CAS No.

130641-38-2

SMILES

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

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
In Vitro: 

DMSO : ≥ 46 mg/mL (141.81 mM)

*"≥" means soluble, but saturation unknown.

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.83%

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Bindarit
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HY-B0498
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