SML0020

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

Propriétés

• Essai: ≥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
• Chaîne SMILES: 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
• Clé InChI: XQYASZNUFDVMFH-CQSZACIVSA-N

Description

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.[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]

Actions biochimiques/physiologiques

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.

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.

Informations sur la sécurité

• 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