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CY-09

产品编号 T4164 CAS 1073612-91-5

别名: CY 09

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。

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CY-09, CAS 1073612-91-5

规格	价格/CNY	货期
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

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纯度: 100%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

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

存储

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

溶解度

DMSO: 77 mg/mL(181.8 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	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

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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参考文献

1. Jiang H, et al. Identification of a selective and direct NLRP3 inhibitor to treat inflammatory disorders. J Exp Med. 2017 Nov 6;214(11):3219-3238. 2. Jia Y, Cui R, Wang C, et al. Metformin protects against intestinal ischemia-reperfusion injury and cell pyroptosis via TXNIP-NLRP3-GSDMD pathway[J]. Redox Biology. 2020: 101534. 3. Chen Z, Zhang S, Nie B, et al. Metformin protects against intestinal ischemia-reperfusion injury and cell pyroptosis via TXNIP-NLRP3-GSDMD pathway[J]. Redox Biology. 2020: 101534.

文献引用

1. Jia Y, Cui R, Wang C, et al. Metformin protects against intestinal ischemia-reperfusion injury and cell pyroptosis via TXNIP-NLRP3-GSDMD pathway. Redox Biology. 2020: 101534. 2. Jia Y, Cui R, Wang C, et al. Metformin protects against intestinal ischemia-reperfusion injury and cell pyroptosis via TXNIP-NLRP3-GSDMD pathway. Redox Biology. 2020: 101534. 3. Zhang Y, Liu Y, Xie Z, et al.Inhibition of PFKFB Preserves Intestinal Barrier Function in Sepsis by Inhibiting NLRP3/GSDMD.Oxidative Medicine and Cellular Longevity.2022, 2022. 4. Zhu Q, Zheng F, You W, et al.Expression of histone H1 in rats with traumatic brain injury and the effect of the NLRP3 inflammasome pathway.World Neurosurgery.2022

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

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

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

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。

% DMSO+

% +

% Tween 80+

% ddH₂O

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计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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

CY-09 1073612-91-5 Immunology/Inflammation NF-Κb NOD-like Receptor (NLR) NOD CY09 Inhibitor inhibit CY 09 inhibitor

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CY-09

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

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剂量换算

体内实验配液计算器

技术支持

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