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Cat. No.: HY-110391

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BX-513

Name: BX-513
Brand: MedChemExpress
SKU: HY-110391
Availability: PreOrder

(Synonyms: VUF 2274)

BX-513 (VUF2274) is a CCR1 antagonist that inhibits chemokine binding and blocks US28 signaling. BX-513 inhibits human CCR1 with a K_i 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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CAS No.: 193542-65-3
화학식: C₂₈H₂₉ClN₂O
분자량:445.00

보관:

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

BX-513 Chemical Structure

CAS No.: 193542-65-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[2]

CCR1

40 nM (Ki)

All CCR Isoforms :

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 (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 K_i 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 K_i 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.

Related Protocols :

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 193542-65-3
분자량 445.00
화학식 C₂₈H₂₉ClN₂O
SMILES

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

VUF 2274
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[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.

[3]. Onuffer J, et al. Structure function differences in nonpeptide CCR1 antagonists for human and mouse CCR1. The Journal of Immunology. 2003 Feb;170(4):1910-6.

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

MOQ

Minimum order quantity

100 mg

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- Clinical Trial
Chemical Information
순도&문서
References

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BX-513

All CCR Isoforms