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Tocris/(±)-NBI 74330/4528/10/10 mg

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货号: 4528/10

品牌: Tocris

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Description: Potent and selective CXCR3 antagonist

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

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

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 (Cat. No. 4487).

Compound Libraries

(±)-NBI 74330 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	605.58
Formula	C₃₂H₂₇F₄N₅O₃
Storage	Store at -20°C
Purity	≥98% (HPLC)
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 605.58. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.65 mL	8.26 mL	16.51 mL
5 mM	0.33 mL	1.65 mL	3.3 mL
10 mM	0.17 mL	0.83 mL	1.65 mL
50 mM	0.03 mL	0.17 mL	0.33 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Storelli et al (2007) 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. 340 281 PMID: 17562560

Verzijl et al (2008) Noncompetitive antagonism and inverse agonism as mechanism of action of nonpeptidergic antagonists at primate and rodent CXCR3 chemokine receptors. J.Pharmacol.Exp.Ther. 325 544 PMID: 18270317

Heise et al (2005) Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist. J.Pharmacol.Exp.Ther. 313 1263 PMID: 15761110

Keywords: (±)-NBI 74330, supplier, VUF10472, (±)-NBI74330, potent, selective, CXCR3, antagonists, chemokines, (±)-NBI_74330, Chemokine, CXC, Receptors, Chemokine, CXC, Receptors, Tocris Bioscience

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