BX-513
BX-513 (VUF2274) is a CCR1 antagonist that inhibits chemokine binding and blocks US28 signaling. BX-513 inhibits human CCR1 with a Ki of 40 nM. BX-513 blocks CCL3-mediated signaling/chemotaxis, CCR1-mediated chemokine signaling, calcium mobilization, extracellular acidification, and US28-mediated HIV entry, with an IC50 of 4.9 μM. BX-513 can be used for research on hcmv infection.
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- No. CAS: 193542-65-3
- Fòrmula: C28H29ClN2O
- Peso molecular:445.00
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[2]|
CCR1 40 nM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.63 μM
Compound: 23
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Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
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[PMID: 12166951] |
| CHO | IC50 |
9 μM
Compound: 23
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Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
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[PMID: 12166951] |
| COS-7 | EC50 |
3.2 μM
Compound: 1 table-1
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Effective concentration against US28-mediated inositol phosphate production in COS-7 cells
Effective concentration against US28-mediated inositol phosphate production in COS-7 cells
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[PMID: 16190772] |
| COS-7 | IC50 |
9.3 μM
Compound: 1 table-1
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Inhibitory concentration against chemokine receptor US28 expressed in COS-7 cells using [125I]-CCL5
Inhibitory concentration against chemokine receptor US28 expressed in COS-7 cells using [125I]-CCL5
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[PMID: 16190772] |
| HEK293 | EC50 |
4.5 μM
Compound: VUF2274
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Inverse agonist activity at HCMV TB40/E US28 expressed in human HEK cells assessed as Elk-1 activation preincubated for 1 hrs measured after 20 to 24 hrs by luciferase reporter gene assay
Inverse agonist activity at HCMV TB40/E US28 expressed in human HEK cells assessed as Elk-1 activation preincubated for 1 hrs measured after 20 to 24 hrs by luciferase reporter gene assay
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[PMID: 21784633] |
| HEK293 | IC50 |
2.5 μM
Compound: 6s
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Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
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[PMID: 10579830] |
| HEK-293T | EC50 |
>10 μM
Compound: VUF2274
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Allosteric modulatory activity at FLAG-tagged human cytomegalovirus US28 receptor delta300 mutant expressed in HEK293T cells by PathDetectElk1 assay
Allosteric modulatory activity at FLAG-tagged human cytomegalovirus US28 receptor delta300 mutant expressed in HEK293T cells by PathDetectElk1 assay
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[PMID: 25052428] |
| HEK-293T | EC50 |
4.5 μM
Compound: VUF2274
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Allosteric modulatory activity at FLAG-tagged wild type human cytomegalovirus US28 receptor expressed in HEK293T cells by PathDetectElk1 assay
Allosteric modulatory activity at FLAG-tagged wild type human cytomegalovirus US28 receptor expressed in HEK293T cells by PathDetectElk1 assay
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[PMID: 25052428] |
In Vitro
BX-513 (VUF2274) (Compound 1) (1 h) displaces the binding of [125I]CCL5 to US28 in COS-7 cell membranes with an IC50 of 4.9 µM[1].
BX-513 binds to human CCR1 with a Ki of 40 nM and exhibits species-dependent affinity, showing weaker potency against rabbit, mouse, and marmoset CCR1[2].
BX-513 inhibits MIP-1-induced extracellular acidification and intracellular Ca2+ mobilization in cells expressing human CCR1 with a potency of 40 nM[2].
BX-513 inhibits MIP-1 and RANTES-induced PBMC migration, but does not inhibit MIP-1, MCP-1, or SDF-1-stimulated migration[2].
BX-513 inhibits the binding of radiolabeled human MIP-1α to HEK 293 cells expressing human CCR1 with a Ki of 40 nM, while its potency against mouse CCR1 is approximately 88-fold lower[3].
BX-513 (10 μM) exhibits significant cross-reactivity with adrenergic, dopaminergic, and serotonergic neurotransmitter receptors[2].
BX-513 (2 h) inhibits constitutive [3H]inositol phosphate production in US28-expressing SVEC4-10 cells with an EC50 of 3.2 µM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 193542-65-3
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Peso molecular 445.00
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Fòrmula C28H29ClN2O
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SMILES
N#CC(C=1C=CC=CC1)(C=2C=CC=CC2)CCCN3CCC(O)(C4=CC=C(Cl)C=C4)CC3
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Synonyms
VUF 2274
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Hulshof JW, et al. Synthesis and pharmacological characterization of novel inverse agonists acting on the viral-encoded chemokine receptor US28. Bioorganic & medicinal chemistry. 2006 Nov 01;14(21):7213-30. [Content Brief]
[2]. Horuk R, et al. BX471: a CCR1 antagonist with anti-inflammatory activity in man. Mini reviews in medicinal chemistry. 2005 Sep;5(9):791-804. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BX-513 Related Classifications
HY-110391 Related Classifications
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