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CAS No.: 1073612-91-5

CY-09 Catalog No. CSN21218

Synonyms: N/A

CY-09 can inhibit NLRP3 with Kd value of 500 nM through directly bounding to the ATP-binding site of the NLRP3 NACHT domain.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述NOD-like receptor (NLR) family are a group of inflammasomes formed by innate immune sensors. NLRP3 is a member of NLR family and its aberrant activation is involved in the pathogenesis of a variety of human diseases. CY-09 is a NLRP3 inhibitor that blocks the ATPase activity of the NLRP3 NACHT domain, which is essential for the oligomerization of NLRP3, resulting in the suppression of NLRP3 inflammasome activation. CY-09 shows inhibitory activities against five major cytochrome P450 enzymes 1A2, 2C9, 2C19, 2D6, and 3A4 with IC₅₀ values of 18.9, 8.18, >50, >50, and 26.0 µM, respectively. CY-09 at 1-10 µM dose-dependently inhibited the monosodium urate (MSU), nigericin, ATP-induced caspase-1 activation and IL-1β secretion in LPS-primed BMDMs. Cytosolic LPS-induced noncanonical NLRP3 activation in BMDMs was also inhibited by CY-09 treatment (1-10µM). CY-09 at the doses of 1-10µM effectively suppressed nigericin-induced ASC oligomerization in BMDMs, but showed no effect on nigericin-induced mitochondrial damage and reactive oxygen species production. Treatment with 5-10µM CY-09 in HEK-293T cells inhibited the interaction of Flag–NLRP3 and mCherry–NLRP3, suggesting the inhibitory function of CY-09 on NLRP3 oligomerization. CY-09 inhibited the ATPase activity of purified NLRP3 at doses of 0.1-1µM, and the K_d value between CY-09 and purified GFP-NLRP3 was about 500nM. In a mouse model of cryopyrin-associated autoinflammatory syndrome, treatment of CY-09 (40mg/kg) efficiently suppressed MSU injection-induced IL-1β production and neutrophil influx^[1].
动物研究
剂量
C57BL/6J mice: 5 mg/kg^[1] (i.v.); 10 mg/kg^[1] (p.o.); 40 mg/kg^[1] (i.p.)

给药途径
i.v., p.o., i.p.
参考文献

动物研究
剂量	C57BL/6J mice: 5 mg/kg^[1] (i.v.); 10 mg/kg^[1] (p.o.); 40 mg/kg^[1] (i.p.)
给药途径	i.v., p.o., i.p.

[1] Jiang H, He H, Chen Y, Huang W, Cheng J, Ye J, Wang A, Tao J, Wang C, Liu Q, Jin T, Jiang W, Deng X, Zhou R. Identification of a selective and direct NLRP3 inhibitor to treat inflammatory disorders. J Exp Med. 2017 Nov 6;214(11):3219-3238. doi: 10.1084/jem.20171419. Epub 2017 Oct 11. PMID: 29021150; PMCID: PMC5679172.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3617 mL
- 11.8084 mL
- 23.6167 mL
- 5 mM
- 0.4723 mL
- 2.3617 mL
- 4.7233 mL
- 10 mM
- 0.2362 mL
- 1.1808 mL
- 2.3617 mL

技术信息

CAS号

1073612-91-5

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H12F3NO3S2

运输

蓝冰

分子量

423.43

别名

N/A

溶解度

DMSO	50.0 mg/mL (118.1 mM)

动物实验配方

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CY-09 Catalog No. CSN21218

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