[CAS NO. 130641-38-2] Bindarit

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PRODUCTS SPECIFICATIONS [130641-38-2]

Catalog

HY-B0498

Brand

MCE

CAS

130641-38-2

DESCRIPTION [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

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

12 Publications Citing Use of MCE

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

Source

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 available by MCE.