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NBI-74330

Catalog No: 6111112
CAS Number: 855527-92-3
Purity: 98% 

NBI-74330 is a small molecule antagonist for CXCR3, NBI-74330 demonstrates potent inhibition of [(125)I]CXCL10 and [(125)I]CXCL11 specific binding (K(i) of 1.5 and 3.2 nM, respectively.

NBI-74330 demonstrated potent inhibition of [(125)I]CXCL10 and [(125)I]CXCL11 specific binding (K(i) of 1.5 and 3.2 nM, respectively) and of functional responses mediated by CXCR3, such as ligand-induced guanosine 5'-O-(3-[(35)S]thio)triphosphate ([(35)S]GTPgammaS) binding, calcium mobilization, and cellular chemotaxis (IC(50) of 7 to 18 nM). NBI-74330 was selective for CXCR3 because it showed no significant inhibition of chemotactic responses to other chemokines and did not inhibit radioligand binding to a panel of nonchemokine G-protein coupled receptors. There was a striking difference in potencies among the three CXCR3 ligands, with CXCL11 >> CXCL10 > CXCL9 [1]. The affinity of a small molecule CXCR3 antagonist, NBI-74330, was obtained in the absence or presence of plasma (buffer pA2 value: 7.84+/-0.14; plasma pKB) value 6.36+/-0.01) [2].

 

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Chemical Information

NameNBI-74330
Iupac Chemical NameNBI-74330 
SynonymsNBI 74330; NBI74330 
Molecular FormulaC32H27F4N5O3 
Molecular Weight605.58 
SmileCCOc1ccc(cc1)n2c(=O)c3cccnc3nc2C(C)N(Cc4cccnc4)C(=O)Cc5ccc(c(c5)C(F)(F)F)F
InChiKeyXMRGQUDUVGRCBS-UHFFFAOYSA-N
InChiInChI=1S/C32H27F4N5O3/c1-3-44-24-11-9-23(10-12-24)41-30(39-29-25(31(41)43)7-5-15-38-29)20(2)40(19-22-6-4-14-37-18-22)28(42)17-21-8-13-27(33)26(16-21)32(34,35)36/h4-16,18,20H,3,17,19H2,1-2H3
CAS Number855527-92-3
MDLMFCD22665718
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Ordering Information

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Formulationcrystalline solid 
Purity98% 
Storage3 years -20ºCpowder 
SolubilitySoluble in DMSO 
Handling
Shipping ConditionShipped under ambient temperature as non-hazardous chemical. 
HS Code
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Targets
Mechanism
Cell study
Animal study
Clinical study
Not available

Chemical Structure

6111112 - NBI-74330 | CAS 855527-92-3

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