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Merck

SML0020

Sigma-Aldrich

BX471

≥98% (HPLC)

Synonym(e):

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

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5 MG
168,00 €
25 MG
565,00 €

168,00 €


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5 MG
168,00 €
25 MG
565,00 €

About This Item

Empirische Formel (Hill-System):
C21H24ClFN4O3
CAS-Nummer:
Molekulargewicht:
434.89
UNSPSC-Code:
51111800
NACRES:
NA.77

168,00 €


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Qualitätsniveau

Assay

≥98% (HPLC)

Form

powder

Lagerbedingungen

desiccated

Farbe

white to tan

Löslichkeit

DMSO: ≥25 mg/mL

Ersteller

Bayer

Lagertemp.

2-8°C

SMILES String

Fc1ccc(cc1)CN2C[C@H](N(CC2)C(=O)COc3c(cc(cc3)Cl)NC(=O)N)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

InChIKey

XQYASZNUFDVMFH-CQSZACIVSA-N

Anwendung

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.[1] It has also been used as a CCR1 inhibitor to assess the effects of CCR1 on the migration and epithelial-mesenchymal transition (EMT).[2]

Biochem./physiol. Wirkung

BX471 blocks CCR1 and downregulates the mRNA expression of ICAM-1, P-selectin and E-selectin.[3] It decreases the inflammatory responses in sepsis,[3] prevents monocyte recruitment in inflammation sites in rheumatoid arthritis patients[4] and inhibits interstitial leukocyte recruitment and fibrosis in mouse model of lupus nephritis.[5]
BX471 is a CCR1 Antagonist
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.

Leistungsmerkmale und Vorteile

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.

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable


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Die Dokumentenbibliothek aufrufen

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
Min He et al.
American journal of physiology. Gastrointestinal and liver physiology, 292(4), G1173-G1180 (2007-01-20)
Sepsis is a complex clinical syndrome resulting from a harmful host inflammatory response to infection. Chemokines and their receptors play a key role in the pathogenesis of sepsis. BX471 is a potent nonpeptide CC chemokine receptor-1 (CCR1) antagonist in both

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