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Merck
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Key Documents

SML0020

Sigma-Aldrich

BX471

≥98% (HPLC)

Synonyme(s) :

N-[5-chloro-2-[2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methyl-1-piperazinyl]-2-oxoethoxy]phenyl]-urea, ZK-811752

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About This Item

Formule empirique (notation de Hill):
C21H24ClFN4O3
Numéro CAS:
217645-70-0
Poids moléculaire :
434.89
Code UNSPSC :
51111800
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Conditions de stockage

desiccated

Couleur

white to tan

Solubilité

DMSO: ≥25 mg/mL

Auteur

Bayer

Température de stockage

2-8°C

InChI

1S/C21H24ClFN4O3/c1-14-11-26(12-15-2-5-17(23)6-3-15)8-9-27(14)20(28)13-30-19-7-4-16(22)10-18(19)25-21(24)29/h2-7,10,14H,8-9,11-13H2,1H3,(H3,24,25,29)/t14-/m1/s1

Clé InChI

XQYASZNUFDVMFH-CQSZACIVSA-N

Application

BX471 has been used in chemotaxis assay to study the responses of HEK293 cells expressing human C-C motif chemokine receptor 1 (CCR1) to CC motif ligand 3 (CCL3)-induced cell migration. It has also been used as a CCR1 inhibitor to assess the effects of CCR1 on the migration and epithelial-mesenchymal transition (EMT).

Actions biochimiques/physiologiques

BX471 blocks CCR1 and downregulates the mRNA expression of ICAM-1, P-selectin and E-selectin. It decreases the inflammatory responses in sepsis, prevents monocyte recruitment in inflammation sites in rheumatoid arthritis patients and inhibits interstitial leukocyte recruitment and fibrosis in mouse model of lupus nephritis.
BX471 is an orally active, CCR-1 specific antagonist. It displaces the endogenous CCR-1 ligands MIP-1a, RANTES and MCP-3 (Ki range 1-5 nM). BX471 inhibits CCR-1 effects in leukocytes, including calcium mobilization and migration.

Caractéristiques et avantages

This compound is featured on the Chemokine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Bayer. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

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Consulter la Bibliothèque de documents

Human MSCs promotes colorectal cancer epithelial-mesenchymal transition and progression via CCL5beta-catenin Slug pathway
Chen K, et al.
Cell Death & Disease, 8(5), e2819-e2819 (2017)
Maria C Lebre et al.
PloS one, 6(7), e21772-e21772 (2011-07-13)
The aim of this study was to provide more insight into the question as to why blockade of CCR1, CCR2, and CCR5 may have failed in clinical trials in rheumatoid arthritis (RA) patients, using an in vitro monocyte migration system
The role of CCR1 and therapeutic effects of anti-CCL3 antibody in herpes simplex virus-induced Behccet's disease mouse model
Sayeed HM, et al.
Immunology (2019)
Hans-Joachim Anders et al.
Journal of the American Society of Nephrology : JASN, 15(6), 1504-1513 (2004-05-22)
Slowly progressive renal injury is the major cause for ESRD. The model of progressive immune complex glomerulonephritis in autoimmune MRL(lpr/lpr) mice was used to evaluate whether chemokine receptor CCR1 blockade late in the disease course can affect progression to renal
Nagarajan Vaidehi et al.
The Journal of biological chemistry, 281(37), 27613-27620 (2006-07-14)
A major challenge in the application of structure-based drug design methods to proteins belonging to the superfamily of G protein-coupled receptors (GPCRs) is the paucity of structural information (1). The 19 chemokine receptors, belonging to the Class A family of
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