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Referencia número: HY-110391

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BX-513

(Synonyms: VUF 2274)

BX-513 is a highly potent and selective CCR1 antagonist. BX-513 effectively inhibits the binding of radiolabeled MIP-1α and RANTES to CCR1, with K_i values of 40 nM and 60 nM, respectively. BX-513 suppresses MIP-1α-induced extracellular acidification, MIP-1α- and RANTES-induced intracellular calcium mobilization, as well as MIP-1α- and RANTES-induced migration of peripheral blood mononuclear cells. BX-513 can be used for the research of rheumatoid arthritis and multiple sclerosis.

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No. CAS: 193542-65-3
Fòrmula: C₂₈H₂₉ClN₂O
Peso molecular:445.00

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Please store the product under the recommended conditions in the Certificate of Analysis.

BX-513 Chemical Structure

No. CAS: 193542-65-3

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Descripciòn

Ver todos los productos específicos de isoformas CCR :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.63 μM Compound: 23	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	[PMID: 12166951]
CHO	IC₅₀	9 μM Compound: 23	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	[PMID: 12166951]
COS-7	EC₅₀	3.2 μM Compound: 1 table-1	Effective concentration against US28-mediated inositol phosphate production in COS-7 cells Effective concentration against US28-mediated inositol phosphate production in COS-7 cells	[PMID: 16190772]
COS-7	IC₅₀	9.3 μM Compound: 1 table-1	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	[PMID: 16190772]
HEK293	EC₅₀	4.5 μM Compound: VUF2274	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	[PMID: 21784633]
HEK293	IC₅₀	2.5 μM Compound: 6s	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	[PMID: 10579830]
HEK-293T	EC₅₀	>10 μM Compound: VUF2274	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	[PMID: 25052428]
HEK-293T	EC₅₀	4.5 μM Compound: VUF2274	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	[PMID: 25052428]

In Vitro

BX-513 (Compound 1) (30-1000 nM) dose-dependently inhibits MIP-1α-induced extracellular acidification in THP-1 cells, with an IC₅₀ of 124 nM, and also suppresses RANTES-induced acidification in these cells^[1].
BX-513 (100-1000 nM) inhibits CCR1-expressing HEK 293 cells in a dose-dependent manner, with an IC₅₀ of approximately 200 nM. This compound has no intrinsic agonist activity, exerts reversible inhibitory effects, and also inhibits RANTES-induced intracellular Ca²⁺ mobilization in these cells^[1].
BX-513 (20-2000 nM) dose-dependently inhibits MIP-1α- and RANTES-induced chemotaxis of human peripheral blood mononuclear cells (PBMCs), without affecting migration induced by other chemokines^[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 A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 193542-65-3
Peso molecular 445.00
Fòrmula C₂₈H₂₉ClN₂O
SMILES

N#CC(C=1C=CC=CC1)(C=2C=CC=CC2)CCCN3CCC(O)(C4=CC=C(Cl)C=C4)CC3
Synonyms

VUF 2274
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Hesselgesser J, et al. Identification and characterization of small molecule functional antagonists of the CCR1 chemokine receptor. J Biol Chem. 1998;273(25):15687-15692. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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BX-513

Ver todos los productos específicos de isoformas CCR

Actividad biológica

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Referencias

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BX-513 Related Classifications

HY-110391 Related Classifications