A CXCR3 antagonist (Ki = 3.6 nM in a radioligand binding assay); inhibits CXCL10- or CXCL11-induced calcium mobilization in RBL cells expressing human CXCR3 (IC50 = 7 nM for both); inhibits CXCL11-induced chemotaxis of CXCR3-expressing H9 cells and PHA/IL-2 T cells (IC50s = 3.9 and 6.6 nM

NBI 74330 – 5 mg

Brand:
Cayman
CAS:
855527-92-3
Storage:
-20
UN-No:
Non-Hazardous - /

NBI 74330 is a chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist (Ki = 3.6 nM in a radioligand binding assay).{52169} It inhibits calcium mobilization induced by chemokine (C-X-C motif) ligand 10 (CXCL10) or CXCL11 in RBL cells expressing human CXCR3 (IC50 = 7 nM for both). NBI 74330 inhibits CXCL11-induced chemotaxis of CXCR3-expressing H9 cells and PHA and IL-2 differentiated T cells (IC50s = 3.9 and 6.6 nM, respectively). In vivo, NBI 74330 (100 mg/kg) reduces peritoneal lymphocyte migration in a mouse model of peritonitis.{52170} It reduces the size and number of aortic arch atherosclerotic lesions in Ldlr-/- mice. NBI 74330 reduces spinal cord microglial activation and levels of CXCL4, CXCL9, and CXCL10 and decreases thermal and mechanical hyperalgesia in a rat model of chronic constriction injury-induced neuropathic pain.{52171}  

 

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Description

A CXCR3 antagonist (Ki = 3.6 nM in a radioligand binding assay); inhibits CXCL10- or CXCL11-induced calcium mobilization in RBL cells expressing human CXCR3 (IC50 = 7 nM for both); inhibits CXCL11-induced chemotaxis of CXCR3-expressing H9 cells and PHA/IL-2 T cells (IC50s = 3.9 and 6.6 nM, respectively); reduces peritoneal lymphocyte migration in a mouse model of peritonitis at 100 mg/kg; reduces the size and number of aortic arch atherosclerotic lesions in Ldlr-/- mice; reduces spinal cord microglial activation and levels of CXCL4, CXCL9, and CXCL10 and decreases thermal and mechanical hyperalgesia in a rat model of chronic constriction injury-induced neuropathic pain

Formal name: N-[(1R)-1-[3-(4-ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-4-fluoro-N-(3-pyridinylmethyl)-3-(trifluoromethyl)benzeneacetamide

Synonyms: 

Molecular weight: 605.6

CAS: 855527-92-3

Purity: ≥98%

Formulation: A solid

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