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CS-1298

CS-1298

中文名稱CS-1298
中文同義詞BX471鹽酸鹽;化合物 T14845;(R)-1-(5-氯-2-(2-(4-(4-氟芐基)-2-甲基哌嗪-1-基)-2-氧代乙氧基)苯基)脲 鹽酸鹽;化合物 BX471 HYDROCHLORIDE
英文名稱BX471 (hydrochloride)
英文同義詞BX471 (hydrochloride);N-[5-Chloro-2-[2-[4-(4-fluorobenzyl)-2(R)-methylpiperazin-1-yl]-2-oxoethoxy]phenyl]urea hydrochloride ZK-811752(BX471);CS-1298;BX471 HYDROCHLORIDE;BX-471 HYDROCHLORIDE;BX 471 HYDROCHLORIDE;ZK-811752 hydrochloride;(R)-1-(5-Chloro-2-(2-(4-(4-fluorobenzyl)-2-methylpiperazin-1-yl)-2-oxoethoxy)phenyl)urea hydrochloride;BX471 hydrochloride (BX-471 hydrochloride
CAS號(hào)288262-96-4
分子式C21H25Cl2FN4O3
分子量471.35
EINECS號(hào)
相關(guān)類別
Mol文件288262-96-4.mol
結(jié)構(gòu)式CS-1298 結(jié)構(gòu)式

CS-1298 性質(zhì)

儲(chǔ)存條件under inert gas (nitrogen or Argon) at 2-8°C
溶解度二甲基亞砜:150 mg/ml(318.23 mM)
形態(tài)固體
顏色白色至黃色

CS-1298 用途與合成方法

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(duì)其選擇性是對(duì) CCR2,CCR5 和 CXCR4 的 250 倍。

MIP-1α-CCR1

1 nM (Ki)

RANTES-CCR1

2.8 nM (Ki)

MCP-3-CCR1

5.5 nM (Ki)

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.

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.

安全信息

MSDS信息

更新日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2026/06/05HY-12080ABX471 hydrochloride288262-96-45 mg1025元
2026/06/05HY-12080ACS-1298
BX471 hydrochloride
288262-96-410mM * 1mLin DMSO1063元

CS-1298 上下游產(chǎn)品信息

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