Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BX471 (BX 471) 是可口服的非多肽 CCR1选择性拮抗剂,Ki 值为 1 nM,对其选择性是对 CCR2、CCR5 和 CXCR4 的 250 倍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 297 | 现货 | ||
2 mg | ¥ 438 | 现货 | ||
5 mg | ¥ 683 | 现货 | ||
10 mg | ¥ 1,360 | 现货 | ||
25 mg | ¥ 2,910 | 现货 | ||
50 mg | ¥ 4,280 | 现货 | ||
100 mg | ¥ 6,130 | 现货 | ||
500 mg | ¥ 12,500 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 753 | 现货 |
产品描述 | BX471 (BX 471) is a potent, selective non-peptide CCR1 antagonist. |
靶点活性 | CCR1:1 nM (Ki) |
体外活性 | BX 471 is a potent functional antagonist based on its ability to inhibit a number of CCR1-mediated effects including Ca2+ mobilization, increase in extracellular acidification rate, CD11b expression, and leukocyte migration. BX 471 demonstrats a greater than 10,000-fold selectivity for CCR1 compared with 28 G-protein-coupled receptors[1]. BX471 is also able to displace 125I-MIP-1α/CCL3 binding to mouse CCR1 in a concentration-dependent manner with a Ki of 215±46 nM. Increasing concentrations of BX471 inhibits the Ca2+ transients induced by MIP-1α/CCL3 in both human and mouse CCR1 with IC50 of 5.8±1 nM and 198±7 nM, respectively[2]. 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[4]. |
体内活性 | BX 471 (4 mg/kg, p.o. or i.v.) is orally active with a bioavailability of 60% in dogs. Furthermore, BX 471 effectively reduces disease in a rat experimental allergic encephalomyelitis model of multiple sclerosis[1]. 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[2]. Pretreatment witih BX471 reduces macrophage and neutrophil accumulation in kidney after ischemia-reperfusion injury[3]. |
激酶实验 | Kinase activity assays: In vitro activities of purified GST–NUAK1 and GST–NUAK1[A195T] are measured using Cerenkov counting of incorporation of radioactive 32P from [γ-32P]ATP into Sakamototide substrate peptide. Reactions are carried out in a 50 μL reaction volume for 30 min at 30°C and reactions are terminated by spotting 40 μL of the reaction mix on to P81 paper and immediately immersing in 50 mM orthophosphoric acid. Samples are washed three times in 50 mM orthophosphoric acid followed by a single acetone rinse and air drying. The kinase-mediated incorporation of [γ-32P]ATP into Sakamototide is quantified by Cerenkov counting. One unit of activity is defined as that which catalyses the incorporation of 1 nmol of [32P]phosphate into the substrate over 1 h. |
细胞实验 | Briefly, dermal microvascular endothelial cells grown to confluence in Petri dishes are stimulated with IL-1β (10 ng/mL) for 12 h followed by pre-incubation with RANTES (10 nM) for 30 min at 37°C just prior to assay. The plates are assembled as the lower wall in a parallel wall flow chamber and mounted on the stage of an Olympus IMT-2 inverted microscope with ×20 and ×40 phase-contrast objectives. Isolated human blood monocytes are isolated and resuspended at 5×105?cells/mL in assay buffer (HBSS) containing 10 mM?HEPES, pH 7.4 and 0.5% human serum albumin. Shortly before the assay, 1 mM Mg2+?and 1 mM?Ca2+?are added. The cell suspensions are kept in a heating block at 37°C during the assay and perfused into the flow chamber at a rate of 1.5 dyn/cm2?for 5 min. For inhibition experiments, monocytes are preincubated with BX471 at different concentrations (0.1-10 μM) or a Me2SO control for 10 min at 37°C. The number of firmLy adherent cells after 5 min is quantitated in multiple fields (at least five per experiment) by analysis of images recorded with a long integration JVC 3CCD video camera and a JVC SR L 900 E video recorder and are expressed as cells/mm2. The type of adhesion analyzed is restricted to primary,?i.e.?direct interactions of monocytes with endothelium. |
别名 | BX 471, BX-471, ZK-811752 |
分子量 | 434.89 |
分子式 | C21H24ClFN4O3 |
CAS No. | 217645-70-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100mg/ml(399.4mM), Sonification is recommended
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2994 mL | 11.4972 mL | 22.9943 mL | 57.4858 mL |
5 mM | 0.4599 mL | 2.2994 mL | 4.5989 mL | 11.4972 mL | |
10 mM | 0.2299 mL | 1.1497 mL | 2.2994 mL | 5.7486 mL | |
20 mM | 0.115 mL | 0.5749 mL | 1.1497 mL | 2.8743 mL | |
50 mM | 0.046 mL | 0.2299 mL | 0.4599 mL | 1.1497 mL | |
100 mM | 0.023 mL | 0.115 mL | 0.2299 mL | 0.5749 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
BX471 217645-70-0 Immunology/Inflammation Microbiology/Virology CCR BX 471 CC chemokine receptor Inhibitor BX-471 ZK-811752 inhibit ZK 811752 ZK811752 inhibitor