YQ128|cas:2454246-18-3|西域试剂

YQ128,99.83%

产品编号：Bellancom-130252| CAS NO：2454246-18-3| 分子式：C₂₇H₂₉ClN₂O₄S₂| 分子量：545.11

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-130252	￥1500.00	杭州北京（现货）
Bellancom-130252	￥2500.00	杭州北京（现货）
Bellancom-130252	￥3900.00	杭州北京（现货）
Bellancom-130252	￥6500.00	杭州北京（现货）
Bellancom-130252	￥10500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

YQ128

产品介绍

YQ128 是有效的，选择性第二代 NLRP3 炎性体抑制剂，IC₅₀ 为 0.30 µM。YQ128 能显着和选择性地抑制 IL-1β 的产生，但不抑制 TNF-α 的产生。YQ128 可以穿过血脑屏障到达中枢神经系统。YQ128 具有抗炎活性。

生物活性

YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC₅₀ of 0.30 µM. YQ128 significantly and selectively suppresses the production of IL-1β, but not TNF-α, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity.

体外研究

YQ128 (0.3-100 µM; 30 mins) dose dependently suppressed the release of IL-1β from peritoneal macrophages upon LPS/ATP challenge with an IC₅₀ of 1.59 µM.
YQ128 (20 µM; 2 hours) shows no significant toxic effects on hCMEC/D3 cells.

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

Cell Viability Assay

Cell Line:	Mouse peritoneal macrophages
Concentration:	0.3, 1.0, 3.0, 10, 30, 100 µM
Incubation Time:	30 mins
Result:	Suppressed the release of IL-1β from peritoneal macrophages upon LPS/ATP challenge with an IC₅₀ of 1.59 µM.

体内研究
(In Vivo)

YQ128 (iv; 20 mg/kg) has an intermediate terminal plasma half-life (t_1/2) of 6.6 hours after iv administration.
YQ128 (oral; 20 mg/kg) shows delayed gastrointestinal absorption with a t_max and c_max of 12 h and 73 ng/mL, respectively. Oral bioavailability (F_oral) is estimated as 10%.
YQ128 exhibits extensive extravascular distribution with a large steady-state volume of distribution (Vd_ss) of 8.5 L/kg and rapid total clearance (CL_tot) of 41 mL/min/kg.
YQ128 (10 mg/kg) has been shown to trigger IL-1β production in a NLRP3- dependent manner in C57BL/6 mice.

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

Animal Model:	Sprague-Dawley rats (200-250 g)
Dosage:	20 mg/kg (Pharmacokinetic Analysis)
Administration:	Iv
Result:	Had an intermediate terminal plasma half-life (t_1/2) of 6.6 hours after iv administration.

体内研究

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

Animal Model:	Sprague-Dawley rats (200-250 g)
Dosage:	20 mg/kg (Pharmacokinetic Analysis)
Administration:	Iv
Result:	Had an intermediate terminal plasma half-life (t_1/2) of 6.6 hours after iv administration.

体内研究

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

Animal Model:	Sprague-Dawley rats (200-250 g)
Dosage:	20 mg/kg (Pharmacokinetic Analysis)
Administration:	Iv
Result:	Had an intermediate terminal plasma half-life (t_1/2) of 6.6 hours after iv administration.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (458.62 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8345 mL	9.1725 mL	18.3449 mL
5 mM	0.3669 mL	1.8345 mL	3.6690 mL
10 mM	0.1834 mL	0.9172 mL	1.8345 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.82 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.82 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.82 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.82 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。