SML0020

BX471

≥98% (HPLC)

• 別名: N-[5-chloro-2-[2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methyl-1-piperazinyl]-2-oxoethoxy]phenyl]-urea, ZK-811752
• 実験式（ヒル表記法）: C₂₁H₂₄ClFN₄O₃
• CAS番号: 217645-70-0
• 分子量: 434.89
• UNSPSCコード: 51111800
• NACRES: NA.77

特性

• アッセイ: ≥98% (HPLC)
• フォーム: powder
• 保管条件: desiccated
• 色: white to tan
• 溶解性: DMSO: ≥25 mg/mL
• オーガナイザー: Bayer
• 保管温度: 2-8°C
• SMILES記法: 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

詳細

アプリケーション

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]

生物化学的／生理学的作用

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.

特徴および利点

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.

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable