货号	规格	价格	上海	北京	珠海	重庆	武汉
S88262-2mg买3赠1	98.00%	￥408.00 S88262-2mg ￥408.00 现货（买3赠1）	6 6	-	-	-	-
S88262-5mg买3赠1	98.00%	￥740.00 S88262-5mg ￥740.00 现货（买3赠1）	10 10	-	-	-	-
S88262-10mg买3赠1	98.00%	￥920.00 S88262-10mg ￥920.00 现货（买3赠1）	7 7	-	-	-	-
S88262-25mg买3赠1	98.00%	￥1650.00 S88262-25mg ￥1650.00 现货（买3赠1）	5 5	-	-	-	-
S88262-50mg买3赠1	98.00%	￥2770.00 S88262-50mg ￥2770.00 现货（买3赠1）	6 6	-	-	-	-
S88262-100mg买3赠1	98.00%	￥4500.00 S88262-100mg ￥4500.00 现货（买3赠1）	4 4	-	-	-	-

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产品描述：

CY-09是一种特异的NLRP3 inflammasome的抑制剂，直接靶向NLRP3。它对5种主要的cytochrome P450酶的IC50值分别为18.9, 8.18, >50, >50 和 26.0 µM

靶点：

NLRP3 inflammasome;NOD-likeReceptor(NLR); NOD

体外研究：

CY-09 specifically blocks NLRP3 activation in macrophages. CY-09 inhibits NLRP3 oligomerization and inflammasome assembly. CY-09 directly binds to NLRP3 and inhibits its ATPase activity. The metabolic stability of CY-09 was first evaluated using human and mouse liver microsomes, exhibiting favorable stability with the half-life >145 min for both human and mouse microsomes. The metabolic stability of CY-09 was first evaluated using human and mouse liver microsomes, exhibiting favorable stability with the half-life >145 min for both human and mouse microsomes, which exhibited low risk of drug-drug interactions

体内研究：

CY-09 inhibits NLRP3 activation in vivo and prevents neonatal lethality in a mouse model of CAPS. In pharmacokinetic studies evaluted in C57BL/6J mice administered a single i.v. or oral dose, CY-09 exhibits favorable pharmacokinetics, with a half-life of 2.4 h, an area under the curve of 8,232 (h·ng)/ml, and bioavailability of 72%. CY-09 reverses metabolic disorders in diabetic mice by inhibition of NLRP3-dependent inflammation. CY-09 treatment has remarkable beneficial effects for metainflammation, hyperglycemia, and insulin resistance in diabetic mice

细胞实验：

Cell lines: BMDMs and PBMCs Concentrations: 1, 5, and 10 μM Incubation Time: 30 min Method: 5 × 105/ml BMDMs and 6 × 106/ml PBMCs were plated in 12-well plates. The following morning, the medium was replaced, and cells were 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 were added into the culture for another 30 min, and then the cells were stimulated for 4 h with MSU (150 µg/ml), Salmonella typhimurium (multiplicity of infection) or for 30 min with ATP (2.5 mM) or nigericin (10 µM). Cells were transfected with poly(dA:dT) (0.5 µg/ml) for 4 h or LPS (500 ng/ml) overnight. Cell extracts and precipitated supernatants were analyzed by immunoblot.

动物实验：

Animal Models: C57BL/6J mice Dosages: 5 and 10 mg/kg Administration: i.v. and oral administration

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, 214(11):3219-3238.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.362 ml	11.808 ml	23.617 ml
5 mM	0.472 ml	2.362 ml	4.723 ml
10 mM	0.236 ml	1.181 ml	2.362 ml
50 mM	0.047 ml	0.236 ml	0.472 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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