(±)-NBI 74330

Name: (±)-NBI 74330
Brand: Tocris Bioscience
SKU: 4528

Tocris Bioscience, part of Bio-Techne | Catalog # 4528

Citations (12)

COA / SDS

Potent and selective CXCR3 antagonist

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Product Description
Product Specifications
Solubility
Preparing Stock Solutions
Calculators
Background References
Product Documents
Specific Notices

Key Product Details

Description

Potent and selective CXCR3 antagonist

View all Chemokine Receptor Antagonists »

Product Description

(±)-NBI 74330 is a potent and selective CXCR3 antagonist; potently inhibits ¹²⁵I-CXCL10 binding to CXCR3 (pK_i = 8.13). Inhibits calcium mobilization in response to CXCL11 and CXCL10 in RBL cells. Exhibits no significant effect on chemotaxis induced by CXCR4 or CCR7. Displays a five-fold greater affinity for CXCR3 than (±)-AMG 487.

This product is racemic.

Product Specifications

Molecular Weight

605.58

Formula

C₃₂H₂₇F₄N₅O₃

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

N-1-[(3-4(-Ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-4-fluoro-N-(3-pyridinylmethyl)-3-(trifluoromethyl)benzeneacetamide

CAS Number

473722-68-8

PubChem ID

10167713

InChI Key

XMRGQUDUVGRCBS-UHFFFAOYSA-N

SMILES

CCOC(C=C3)=CC=C3N2C(C1=CC=CN=C1N=C2C(N(CC4=CC=CN=C4)C(CC5=CC(C(F)(F)F)=C(F)C=C5)=O)C)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	30.28	50

Preparing Stock Solutions for (±)-NBI 74330

The following data is based on the product molecular weight 605.58

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.5 mM	3.30 mL	16.51 mL	33.03 mL
2.5 mM	0.66 mL	3.30 mL	6.61 mL
5 mM	0.33 mL	1.65 mL	3.30 mL
25 mM	0.07 mL	0.33 mL	0.66 mL

Calculators

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Background References

References are publications that support the biological activity of the product.

Verzijl Noncompetitive antagonism and inverse agonism as mechanism of action of nonpeptidergic antagonists at primate and rodent CXCR3 chemokine receptors. J.Pharmacol.Exp.Ther. 2008 PMID: 18270317
Heise Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist. J.Pharmacol.Exp.Ther. 2005 PMID: 15761110
Storelli Synthesis and structure-activity relationships of 3H-quinazolin-4-ones and 3H-pyrido[2,3-d]pyrimidin-4-ones as CXCR3 receptor antagonists. Arch.Pharm. 2007 PMID: 17562560