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288262-96-4

中文名稱 CS-1298
英文名稱 BX471 (hydrochloride)
CAS 288262-96-4
更新日期 2025/02/05 16:39:31
分子式 C21H25Cl2FN4O3
分子量 471.35
MOL 文件 288262-96-4.mol
288262-96-4 結(jié)構(gòu)式 288262-96-4 結(jié)構(gòu)式

基本信息

中文別名
BX471鹽酸鹽
英文別名
CS-1298
BX471 (hydrochloride)
ZK-811752 hydrochloride
BX471 HYDROCHLORIDE
BX-471 HYDROCHLORIDE
BX 471 HYDROCHLORIDE
N-[5-Chloro-2-[2-[4-(4-fluorobenzyl)-2(R)-methylpiperazin-1-yl]-2-oxoethoxy]phenyl]urea hydrochloride ZK-811752(BX471)

物理化學(xué)性質(zhì)

儲存條件Inert atmosphere,2-8°C
溶解度DMSO: 150 mg/mL (318.23 mM)
形態(tài)Solid
顏色White to yellow
CS-1298價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2025/02/05HY-12080ABX471 hydrochloride288262-96-45 mg1025元
2025/02/05HY-12080ACS-1298
BX471 hydrochloride
288262-96-410mg1640元
2025/02/05HY-12080ACS-1298
BX471 hydrochloride
288262-96-410mM * 1mLin DMSO1804元

常見問題列表

生物活性
BX471 hydrochloride (ZK-811752 hydrochloride) 是以一種有效的,選擇性的,非肽段的 CCR1 拮抗劑,抑制人 CCR1 活性,Ki 值為 1 nM,對其選擇性是對 CCR2,CCR5 和 CXCR4 的 250 倍。
靶點

MIP-1α-CCR1

1 nM (Ki)

RANTES-CCR1

2.8 nM (Ki)

MCP-3-CCR1

5.5 nM (Ki)

體外研究

BX471 is a potent functional antagonist based on its ability to inhibit a number of CCR1-mediated effects including Ca 2+ mobilization, increase in extracellular acidification rate, CD11b expression, and leukocyte migration. BX471 demonstrats a greater than 10,000-fold selectivity for CCR1 compared with 28 G-protein-coupled receptors. BX471 is also able to displace 125 I-MIP-1α/CCL3 binding to mouse CCR1 in a concentration-dependent manner with a K i of 215±46 nM. Increasing concentrations of BX471 inhibits the Ca 2+ transients induced by MIP-1α/CCL3 in both human and mouse CCR1 with IC 50 of 5.8±1 nM and 198±7 nM, respectively. BX471 (0.1-10 μM) shows a dose-dependent inhibition of RANTES-mediated and shear-resistant adhesion on IL-1β-activated microvascular endothelium in shear flow in isolated blood monocytes. BX471 also inhibits the RANTES-mediated adhesion of T lymphocytes to activated endothelium.

體內(nèi)研究

BX471 (4 mg/kg, p.o. or i.v.) is orally active with a bioavailability of 60% in dogs. Furthermore, BX471 effectively reduces disease in a rat experimental allergic encephalomyelitis model of multiple sclerosis. BX471 (20 mg/kg, s.c.) reaches peak plasma levels of 9 μM by around 30 minutes, and this rapidly declines to approximately 0.4 μM after 2 hours. From 4 to 8 hours the drug plasma levels drops to 0.1 μM or lower. Mice treated with 20 mg/kg of BX471 for 10 days shows a reduction of interstitial CD45 positive leukocytes of approximately 55%. BX471 has a borderline significant effect on the number of CCR5-positive CD8 cells in the peripheral blood. BX471 reduces the amount of FSP1-positive cells by 65% in UUO kidneys as compared with vehicle control. Pretreatment witih BX471 reduces macrophage and neutrophil accumulation in kidney after ischemia-reperfusion injury.

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