货号:A434794
同义名:
ZK-811752; BAY 865047
BX471 is a potent, selective non-peptide CCR1 antagonist (Ki = 1 nM for human CCR1) and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
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描述 | BX471 is a potent and selective non-peptide CCR1 (CC Chemokine Receptor-1). It competitively displaced the CCR1 ligands MIP-1α, RANTES and MCP-3 with Ki values ranging in 1-5.5nM. BX471 could inhibit a number of CCR1-mediated effects including MIP-1α-induced Ca2+ mobilization, increase in extracellular acidification rate, MIP-1α-inducedCD11b expression, and leukocyte and monocyte migration induced by MIP-1α and RANTES. It effectively reduced disease in a rat experimental allergic encephalomyelitis model of multiple sclerosis at doses of 20mg/kg and 50mg/kg[2]. |
作用机制 | BX471 can display CCR1 ligands in a competitive manner.[2] |
Dose | Mice: 3 mg/kg -30 mg/kg[2] (i.p.); 20 mg/kg[3] (s.c.), 100 mg/kg17234893s (s.c.) |
Administration | i.p., s.c. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.30mL 0.46mL 0.23mL |
11.50mL 2.30mL 1.15mL |
22.99mL 4.60mL 2.30mL |
CAS号 | 217645-70-0 |
分子式 | C21H24ClFN4O3 |
分子量 | 434.89 |
SMILES Code | O=C(N)NC1=CC(Cl)=CC=C1OCC(N2[C@H](C)CN(CC3=CC=C(F)C=C3)CC2)=O |
MDL No. | MFCD09859709 |
别名 | ZK-811752; BAY 865047; SH T 04268H |
运输 | 蓝冰 |
InChI Key | XQYASZNUFDVMFH-CQSZACIVSA-N |
Pubchem ID | 512282 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere, 2-8°C |