SML0020
BX471
≥98% (HPLC)
别名:
N-[5-chloro-2-[2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methyl-1-piperazinyl]-2-oxoethoxy]phenyl]-urea, ZK-811752
产品名称
BX471, ≥98% (HPLC)
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
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to tan
solubility
DMSO: ≥25 mg/mL
originator
Bayer
storage temp.
2-8°C
Quality Level
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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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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