SML0020
BX471
≥98% (HPLC)
Synonym(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
Empirical Formula (Hill Notation):
C21H24ClFN4O3
CAS Number:
Molecular Weight:
434.89
UNSPSC Code:
51111800
NACRES:
NA.77
Quality Level
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to tan
solubility
DMSO: ≥25 mg/mL
originator
Bayer
storage temp.
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
InChI key
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).
Biochem/physiol Actions
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 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.
Features and Benefits
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.
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Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Articles
We offer many products related to chemokine receptors for your research needs.
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)
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)
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
Global Trade Item Number
| SKU | GTIN |
|---|---|
| SML0020-5MG | 04061833221549 |
| SML0020-25MG | 04061833221532 |