产品货号：
M08158
中文名称：
NLRP3炎症小体抑制剂(YQ128)
英文名称：
产品规格：
1mL(10mM)|5mg|10mg|50mg|100mg
发货周期：
1～3天
产品价格：
询价
YQ128是有效的，选择性第二代NLRP3炎性体抑制剂，IC50为0.30μM。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。
本产品仅用作科学研究，严禁用于临床治疗等其他非科研用途。
相关搜索：NLRP3炎症小体抑制剂(YQ128)，IL-1β产生抑制剂
本产品仅用作科学研究，严禁用于临床治疗等其他非科研用途。
| IC50 & Target | NLRP3 | IL-1β | ||||||||||||||||
| 0.30μM (IC50) | ||||||||||||||||||
| In Vitro | YQ128 (0.3-100μM;30 mins) dose dependently suppressed the release of IL-1β from peritoneal macrophages upon LPS/ATP challenge with an IC50 of 1.59μM. YQ128 (20μM;2hours) shows no significant toxic effects on hCMEC/D3 cells. Cell Viability Assay | |||||||||||||||||
| Cell Line: | Mouse peritoneal macrophages | |||||||||||||||||
| Concentration: | 0.3,1.0,3.0,10,30,100μM | |||||||||||||||||
| Incubation Time: | 30 mins | |||||||||||||||||
| Result: | Suppressed the release of IL-1β from peritoneal macrophages upon LPS/ATP challenge with an IC50 of 1.59μM. | |||||||||||||||||
| In Vivo | YQ128 (iv;20mg/kg) has an intermediate terminal plasma half-life (t1/2) of 6.6hours after iv administration. YQ128 (oral;20mg/kg) shows delayed gastrointestinal absorption with a tmax and cmax of 12h and 73ng/mL,respectively.Oral bioavailability (Foral) is estimated as 10%. YQ128 exhibits extensive extravascular distribution with a large steady-state volume of distribution (Vdss) of 8.5L/kg and rapid total clearance (CLtot) of 41mL/min/kg. YQ128 (10mg/kg) has been shown to trigger IL-1β production in a NLRP3- dependent manner in C57BL/6 mice. | |||||||||||||||||
| Animal Model: | Sprague-Dawley rats (200-250g) | |||||||||||||||||
| Dosage: | 20mg/kg (Pharmacokinetic Analysis) | |||||||||||||||||
| Administration: | Iv | |||||||||||||||||
| Result: | Had an intermediate terminal plasma half-life (t1/2) of 6.6hours after iv administration. | |||||||||||||||||
| Molecular Weight | 545.11 | |||||||||||||||||
| Formula | C27H29ClN2O4S2 | |||||||||||||||||
| Purity | 99.65% | |||||||||||||||||
| SMILES | O=S(C1=CC=C(CCN(CC2=C(C=CC(Cl)=C2)OCCC)C(CC3=CSC=C3)=O)C=C1)(NCC#C)=O | |||||||||||||||||
| Storage | Powder | -20℃ 3 years | ||||||||||||||||
| 4℃ 2 years | ||||||||||||||||||
| In solvent | -80℃ 6 months | |||||||||||||||||
| -20℃ 1 month | ||||||||||||||||||
| Solvent & Solubility | In Vitro: DMSO:250mg/mL (458.62mM;Need ultrasonic) Preparing Stock Solutions
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℃,6 months;-20℃,1 month。-80℃储存时，请在6个月内使用，-20℃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。
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相关搜索：NLRP3炎症小体抑制剂(YQ128)，IL-1β产生抑制剂