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LIT927

LIT927

产品编号 T5207   CAS 2172879-52-4
别名: LIT 927, LIT-927

LIT927 (LIT-927) 是一种具有口服活性的 CXCL12 中性配体(对于 CXCL12 与 CXCR4 的结合,Ki:267 nM)。

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LIT927 Chemical Structure
LIT927, CAS 2172879-52-4
规格 价格/CNY 货期 数量
1 mg ¥ 278 现货
2 mg ¥ 393 现货
5 mg ¥ 659 现货
10 mg ¥ 987 现货
25 mg ¥ 1,970 现货
50 mg ¥ 2,930 现货
100 mg ¥ 4,260 现货
500 mg ¥ 8,960 现货
1 mL * 10 mM (in DMSO) ¥ 782 现货
产品目录号及名称: LIT927 (T5207)
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纯度: 99.73%
纯度: 99.57%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 LIT927 (LIT-927) is an orally active CXCL12 neutraligand (Ki: 267 nM for CXCL12 binding to CXCR4).
靶点活性 CXCL12:267 nM (Ki)
体外活性 LIT-927 at 10 μM is able to inhibit the increase in intracellular calcium concentration in EGFP-CXCR4+ HEK cells in response to CXCL12, while it has no effect on calcium responses triggered by either CCL17 or CCL22 on EGFP-CCR4+ HEK cells, CCL5 on EGFP-CCR5+ HEK cells, or CCL2 on EGFPCCR2+ HEK cells [1].
体内活性 LIT-927 (350 μmol/kg) inhibited eosinophil infiltration by 54% and 55%. LIT-927 did not exhibit any side effects. In the same murine model of hypereosinophilia, LIT-927 (1400 μmol/kg, P.O.) shows a large and statistically reliable inhibition of eosinophil recruitment (62% inhibition) [1].
细胞实验 HEK EGFP-CXCR4-expressing cells were washed with phosphate-buffered saline (PBS) and detached in PBS-EDTA (5 mM) for 2 min at room temperature. Then cells were carefully resuspended in complete growth medium, pelleted by centrifugation at 320 × g for 5 min, and resuspended in HEPES buffer (137.5 mM NaCl, 6 mM KCl, 1.25 mM CaCl2, 1.25 mM MgCl2, 0.4 mM NaH2PO4, 5.6 mM glucose, 10 mM HEPES (pH 7.4) containing 0.1% BSA. Cells were used at a concentration of 10^6 cells/mL, then the cell suspension (1 mL) was transferred into a quartz cuvette. Time-based recordings of the fluorescence emitted at 510 nm (excitation at 470 nm) were performed at 21 °C using a Fluorolog 3 spectrofluorometer. Fluorescence binding measurements were initiated by adding at t = 150 s, 100 nM CXCL12-Texas Red (TR) to the 1 mL cell suspension. Binding of CXCL12-TR to EGFP-labeled CXCR4 was detected as a reversible decline of emission at 510 nm due to energy transfer from excited EGFP to TR. In the "neutraligand protocol", CXCL12-TR was preincubated for 1 h at room temperature with DMSO or various concentrations of each test compound. Then the premix was added (at t = 150 s), and fluorescence was recorded until equilibrium was reached (300 s). In the "antagonist protocol", DMSO or various concentrations of each test compound were added to EGFP-CXCR4-expressing cells at t = 50 s. Then CXCL12-Texas Red (100 nM) was added at t = 150 s, and fluorescence was recorded until equilibrium was reached (300 s). Dose-response curves of inhibition of CXCL12-TR binding were performed, and the inhibitory constants (Ki) of the different compounds were determined. T134 (20 μM), the CXCR4 receptor antagonist, was used as a control in both "neutraligand" and "antagonist" protocols.
动物实验 The activity of each compound was assessed in vivo in an 8 day model of allergic eosinophilic airway inflammation as described previously. Briefly, 9 week-old male Balb/c mice were sensitized by intraperitoneal injection of 50 μg of ovalbumin adsorbed on 2 mg of aluminum hydroxide in 0.1 mL of saline on days 0, 1, and 2. Mice were challenged intranasally [10 μg of OVA in 25 μL of saline (12.5 μL/nostril)] on days 5, 6, and 7. Control mice received intranasal administration of saline alone. Intranasal administrations were performed under anesthesia with intraperitoneal injection of ketamine (50 mg/kg) and xylazine (3.33 mg/kg). Food and water were supplied ad libitum. Two hours before each OVA or saline challenge, compounds in PBS/Cdx were administered intranasally (12.5 μL/nostril), intraperitoneally, or per os as indicated in the figure legends. Bronchoalveolar lavage (BAL) was performed 24 h after the last OVA or saline challenge as described. Mice were deeply anesthetized by intraperitoneal injection of ketamine (150 mg/kg) and xylazine (10 mg/kg). A plastic cannula was inserted into the trachea, and airways were lavaged by 10 instillations of 0.5 mL of ice-cold saline supplemented with 2.6 mM EDTA (saline-EDTA). BAL fluids were centrifuged (300g, 5 min, 4 °C) to pellet cells, and erythrocytes were lysed by hypotonic shock. Cells were resuspended in 500 μL of icecold saline-EDTA, and total cell counts were determined on a hemocytometer. Differential cell counts were assessed on cytological preparations spanning 250 000 cells/mL in ice-cold saline?EDTA, stained with Diff-Quick with counts of at least 400 cells. Counts were expressed as absolute cell numbers or percentage of inhibition of eosinophil recruitment.
别名 LIT 927, LIT-927
分子量 328.75
分子式 C17H13ClN2O3
CAS No. 2172879-52-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: Insoluble

DMSO: 25 mg/mL (76.05 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0418 mL 15.2091 mL 30.4183 mL 76.0456 mL
5 mM 0.6084 mL 3.0418 mL 6.0837 mL 15.2091 mL
10 mM 0.3042 mL 1.5209 mL 3.0418 mL 7.6046 mL
20 mM 0.1521 mL 0.7605 mL 1.5209 mL 3.8023 mL
50 mM 0.0608 mL 0.3042 mL 0.6084 mL 1.5209 mL

计算器

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参考文献

1. Regenass P, et al. Discovery of a Locally and Orally Active CXCL12 Neutraligand (LIT-927) with Anti-inflammatory Effect in a Murine Model of Allergic Airway Hypereosinophilia. J Med Chem. 2018 Sep 13;61(17):7671-7686.
Navarixin JMS-17-2 Burixafor hydrobromide UNBS5162 WZ811 Baohuoside I Delmetacin Nicotinamide N-oxide

相关化合物库

该产品包含在如下化合物库中:
高选择性抑制剂库 GPCR靶点分子库 细胞因子抑制剂库 抗衰老化合物库 干细胞分化化合物库 已知活性化合物库 自噬库 表型筛选靶点鉴定库 免疫/炎症分子化合物库 经典已知活性库

剂量换算

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体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
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第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

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。

Keywords

LIT927 2172879-52-4 Autophagy GPCR/G Protein Immunology/Inflammation CXCR LIT 927 LIT-927 Inhibitor inhibitor inhibit

 

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