Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CY-09 是NLRP3选择性抑制剂。它能够直接与 NLRP3 NACHT 结构域的 ATP 结合基序结合,对 NLRP3 ATP 酶的活性产生抑制作用,进而抑制 NLRP3 炎症小体的组装和活化。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 413 | 现货 | ||
5 mg | ¥ 745 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,890 | 现货 | ||
50 mg | ¥ 4,270 | 现货 | ||
100 mg | ¥ 5,970 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 822 | 现货 |
产品描述 | CY-09 is an NLRP3 inhibitor. |
体外活性 | CY-09 exhibits a dose-dependent inhibitory effect on monosodium urate (MSU), nigericin, ATP-induced caspase-1 activation and IL-1β secretion at the doses of 1 to10 μM in LPS-primed bone marrow-derived macrophages (BMDMs). Cytosolic LPS-induced noncanonical NLRP3 activation in BMDMs can also be blocked by CY-09 treatment. CY-09 and MCC950 specifically inhibit NLRP3 inflammasome activation and have no effect on LPS-induced priming effects. CY-09 treatment remarkably suppresses nigericin-induced ASC oligomerization. It is found that CY-09 treatment inhibits the interaction of Flag-NLRP3 and mCherry-NLRP3 in HEK-293T cells, suggesting that CY-09 blocks NLRP3 oligomerization |
体内活性 | Compare with MCC950, CY-09 treatment?in vivo?efficiently suppresses monosodium urate (MSU) injection-induced IL-1β production and neutrophil influx, suggesting that CY-09 can block MSU-induced NLRP3 inflammasome activation?in vivo. CY-09 treatment also increases the survival of?NLRP3mutant mice up to days 30 to 48 even after treatment is stopped at day 25. The caspase-1 cleavage observed in adipose tissue of HFD-treated mice is also suppressed by CY-09 |
激酶实验 | For ATPase activity assay, purified recombinant human proteins are incubated at 37°C with indicated concentrations of CY-09 for 15 min in the reaction buffer. ATP (25 μM) is then added, and the mixture is further incubated at 37°C for another 40 min. The amount of ATP converted into adenosine diphosphate (ADP) is determined by luminescent ADP detection with ADP-Glo Kinase Assay kit according to the manufacturer's protocol. The results are expressed as percentage of residual enzyme activity to the vehicle-treated enzyme. For ATP binding assay, purified NLRP3 proteins are incubated with ATP binding agarose for 1 h and then different concentrations of CY-09 are added and incubated for 2 h with motion at 4°C. Beads are washed and boiled in loading buffer. Samples are subjected to immunoblotting analysis[1]. |
细胞实验 | To induce NLRP3 inflammasome activation, 5×105/mL BMDMs and 6×106/mL PBMCs are plated in 12-well plates. The following morning, the medium is replaced, and cells are stimulated with 50 ng/mL LPS or 400 ng/mL Pam3CSK4 (for noncanonical inflammasome activation) for 3 h. After that, CY-09 or other inhibitors are added into the culture for another 30 min, and then the cells are stimulated for 4 h with monosodium urate (MSU) (150 μg/mL),?Salmonella typhimurium?(multiplicity of infection) or for 30 min with ATP (2.5 mM) or nigericin (10 μM). Cells are transfected with poly(dA:dT) (0.5 μg/mL) for 4 h or LPS (500 ng/mL) overnight. Cell extracts and precipitated supernatants are analyzed by immunoblot[1]. |
动物实验 | For the?in vivo?experiments, CY-09 is formulated in a vehicle containing 10% DMSO, 10% Solutol HS 15, and 80% saline,WT or Nlrp3?/? mice at the age of 6 wk, with similar plasma glucose levels and body weights are randomized into different groups. For generation of high-fat diet (HFD)-induced diabetic mice, mice are fed with HFD for 14 wk. The diabetic mice are treated with CY-09 (i.p.) at a dose of 2.5 mg/kg once a day for 6 wk. The mice are maintained with HFD when used for CY-09 treatment and the subsequent experiments[1]. |
别名 | CY 09 |
分子量 | 423.43 |
分子式 | C19H12F3NO3S2 |
CAS No. | 1073612-91-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 77 mg/mL(181.8 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3617 mL | 11.8083 mL | 23.6167 mL | 59.0416 mL |
5 mM | 0.4723 mL | 2.3617 mL | 4.7233 mL | 11.8083 mL | |
10 mM | 0.2362 mL | 1.1808 mL | 2.3617 mL | 5.9042 mL | |
20 mM | 0.1181 mL | 0.5904 mL | 1.1808 mL | 2.9521 mL | |
50 mM | 0.0472 mL | 0.2362 mL | 0.4723 mL | 1.1808 mL | |
100 mM | 0.0236 mL | 0.1181 mL | 0.2362 mL | 0.5904 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。
CY-09 1073612-91-5 Immunology/Inflammation NF-Κb NOD-like Receptor (NLR) NOD CY09 Inhibitor inhibit CY 09 inhibitor