keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ATI-2341 是 C-X-C 趋化因子受体 4 型功能选择性变构激动剂,作为偏向配体有利于 Gα1 激活。它是一种变构激动剂,可激活抑制性异源三聚体 G 蛋白 (Gi) 以促进抑制 cAMP 产生并诱导钙动员。 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 ATI-2341 acetate(1337878-62-2 free base) 的水溶性和稳定性通常比游离态更好。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
100 mg | 待询 | 5日内发货 |
ATI-2341 的其他形式现货产品:
产品描述 | ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. |
靶点活性 | CXCR4:194 nM(EC50) |
体外活性 | ATI-2341 induces CXCR4- and G protein-dependent signaling, receptor internalization, and chemotaxis in CXCR4-expressing cells. It is the most potent agonist with an EC50 value of 194 ± 16 nM and an intrinsic activity of 81 ± 4%. ATI-2341 is a potent and efficacious mobilizer of bone marrow PMNs(polymorphonuclear neutrophils) and HSPCs(hematopoietic stem and progenitor cells) and could represent a previously undescribed therapeutic approach for the recruitment of HSPCs before ABMT(autologous bone marrow transplantation). ATI-2341 is able to induce chemotaxis of CCRF-CEM cells, inducing the typical bell-shaped curve observed with chemotactic agents[1]. |
体内活性 | Intraperitoneal (i.p.) injection of ATI-2341 in BALB/c mice results in a dose-dependent recruitment of PMNs into the peritoneum, with a maximal effect seen at 405 nmol/kg. A higher concentration of ATI-2341 results in reduced recruitment, which is reminiscent of the bell-shaped curve generally seen with chemotactic agents. Intravenous (i.v.) administration of ATI-2341 in mice results in a dose-dependent increase in PMNs in the peripheral circulation, measured 90 min after administration of compound. The effect is maximal at 0.66 μMol/kg of ATI-2341. ATI-2341 has no effect on the mobilization of lymphocytes at any dose tested[1]. |
细胞实验 | Receptors(CXCR4-eGFP) are transiently transfected into HEK-293 cells and are plated 24 h after transfection on glass coverslips coated with poly-D-lysine. The next day, cells are treated with either vehicle alone or with varying concentrations of ATI-2341 for 30 min at 37 °C followed by fixation with methanol for 5 min at −20 °C. GFP fluorescence is visualized directly using a Zeiss Axiovert inverted microscope. Images are processed using Adobe Photoshop and Adobe Illustrator. (Only for Reference) |
别名 | ATI2341 |
分子量 | 2256.82 |
分子式 | C104H178N26O25S2 |
CAS No. | 1337878-62-2 |
keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 2 mg/mL (0.88 mM)
DMSO: 93 mg/mL (41.2 mM)
H2O: <1 mg/mL
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 0.4431 mL | 2.2155 mL | 4.431 mL | 11.0775 mL |
5 mM | 0.0886 mL | 0.4431 mL | 0.8862 mL | 2.2155 mL | |
10 mM | 0.0443 mL | 0.2216 mL | 0.4431 mL | 1.1078 mL | |
20 mM | 0.0222 mL | 0.1108 mL | 0.2216 mL | 0.5539 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。
ATI-2341 1337878-62-2 Autophagy GPCR/G Protein Immunology/Inflammation CXCR Inhibitor inhibit ATI2341 ATI 2341 CXC chemokine receptors inhibitor