NLRP3-IN-10|cas:2641826-39-1|西域试剂

NLRP3-IN-10,98.97%

产品编号：Bellancom-151343| CAS NO：2641826-39-1| 分子式：C₁₇H₁₄BrFO₃| 分子量：365.19

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-151343	￥500.00	杭州北京（现货）
Bellancom-151343	￥800.00	杭州北京（现货）
Bellancom-151343	￥1600.00	杭州北京（现货）
Bellancom-151343	￥2500.00	杭州北京（现货）
Bellancom-151343	￥4000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

NLRP3-IN-10

产品介绍

NLRP3-IN-10 是一种强效的 NLRP3 抑制剂，抑制 IL-1β 的 IC₅₀ 为 251.1 nM。NLRP3-IN-10 能够减弱ASC斑点形成抑制NLRP3炎症小体激活。

生物活性

NLRP3-IN-10 is a potent NLRP3 inhibitor, inhibits IL-1β release with an IC₅₀ value of 251.1 nM. NLRP3-IN-10 suppresses NLRP3 inflammasome activation by attenuating ASC speck formation.

体外研究

NLRP3-IN-10 (compound 14c) (0.4, 1.6, 6.4 μM; 40 min) exerts remarkable inhibitory activity on NLRP3 inflammasome activation induced by LPS-MSU (12 h) in THP-1 cells in a dose-dependent manner.
NLRP3-IN-10 (0.1-6.4 μM; 1.5 h) shows no cytotoxicity against THP-1 cells and (0.1, and 0.4 μM; 40 min) avoids Nigericin (HY-127019)-induced pyroptosis.
NLRP3-IN-10 (0.1, 0.2, and 0.4 μM; 40 min) reduces the processing of caspase-1 p20 and IL-1β, in supernatants in THP-1 cells in a dose-dependent manner.
NLRP3-IN-10 (3 μM and 5 μM; 40 min) decreases LPS-induced THF-α, and (0.2 μM and 0.8 μM; 40 min) reduces the rate of THP-1 cells with ASC specks, indicating ASC oligomerization interruptionsup>.
NLRP3 inflammasome is regarded as a two-step process, including priming and action. NLRP3-IN-10 (1, 10, and 100 μM; 40 min) suppresses LPS-induced NLRP3 priming through directly interacting with NLRP3.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

NLRP3-IN-10 (compound 14c) (10 mg/kg; i.v.; single dose) reduces peritoneal neutrophil influx in mice and IL-1β in the spleen in the MSU-induced peritonitis in LPS-primed mouse model.
NLRP3-IN-10 (10, 30, 90 mg/kg; p.o.; single dose) exhibits extremely low exposure (14.6−23.53 μg·h/L), poor bioavailability (2.47−13.79%), and high plasma clearance (2201.58−5551.12 L/h/kg) after different doses for oral administration.
Pharmacokinetics of NLRP3-IN-10 in mouse

Route	Dose (mg/kg)	AUC_0-t (μg·h/L)	CL (L/h/kg)	C_max (μg/L)	T_1/2 (h)	T_max (h)	F (%)
IV	10	105.88	133.75	81.97	3.13	0.11
PO	10	14.60	2201.58	3.35	7.43	2.11	13.79
PO	30	15.84	2583.27	16.42	7.92	1.26	4.99
PO	90	23.53	5551.12	13.59	6.08	4.21	2.47

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	MSU-induced peritonitis in a LPS-primed mouse model (C57BL/6J mice, 7-week-old, male) LPS: 1 mg/kg, i.p.; MSU: 100 mg/kg, i.v.
Dosage:	10 mg/kg
Administration:	Intravenous injection; single dose
Result:	Significantly reduced IL-1β release in the spleen of mice after 6 h treatment. Significantly reduced the increase of peritoneal neutrophil influx compared with the control group.

体内研究

Route	Dose (mg/kg)	AUC_0-t (μg·h/L)	CL (L/h/kg)	C_max (μg/L)	T_1/2 (h)	T_max (h)	F (%)
IV	10	105.88	133.75	81.97	3.13	0.11
PO	10	14.60	2201.58	3.35	7.43	2.11	13.79
PO	30	15.84	2583.27	16.42	7.92	1.26	4.99
PO	90	23.53	5551.12	13.59	6.08	4.21	2.47

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	MSU-induced peritonitis in a LPS-primed mouse model (C57BL/6J mice, 7-week-old, male) LPS: 1 mg/kg, i.p.; MSU: 100 mg/kg, i.v.
Dosage:	10 mg/kg
Administration:	Intravenous injection; single dose
Result:	Significantly reduced IL-1β release in the spleen of mice after 6 h treatment. Significantly reduced the increase of peritoneal neutrophil influx compared with the control group.