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YQ128 是选择性 NLRP3 炎性体抑制剂(IC50:0.30 µM)。它能显著的、选择性抑制 IL-1β的产生,但不影响 TNF-α 的产生。它能够透过血脑屏障到达中枢神经系统。它具有抗炎作用。
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YQ128 是选择性 NLRP3 炎性体抑制剂(IC50:0.30 µM)。它能显著的、选择性抑制 IL-1β的产生,但不影响 TNF-α 的产生。它能够透过血脑屏障到达中枢神经系统。它具有抗炎作用。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 445 | 现货 | |
2 mg | ¥ 648 | 现货 | |
5 mg | ¥ 1,080 | 现货 | |
10 mg | ¥ 1,680 | 现货 | |
25 mg | ¥ 3,230 | 现货 | |
50 mg | ¥ 4,630 | 现货 | |
100 mg | ¥ 6,480 | 现货 | |
500 mg | ¥ 12,900 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,290 | 现货 |
产品描述 | YQ128 is a potent and selective inhibitor of second-generation NLRP3 (NOD-like receptor P3) inflammasome(IC50 of 0.30 µM), with anti-inflammatory activity. |
靶点活性 | NLRP3:0.30 μM, IL-1β: |
体外活性 | The release of IL-1β from peritoneal macrophages upon LPS/ATP challenge(IC50 of 1.59 μM) dose dependently suppressed by YQ128 (0.3-100 μM; 30 mins). |
体内活性 | YQ128 (oral; 20 mg/kg) shows delayed gastrointestinal absorption with a tmax and cmax of 12 h and 73 ng/mL, respectively. YQ128 exhibits extensive extravascular distribution with a large steady-state volume of distribution (Vdss) of 8.5 L/kg and rapid total clearance (CLtot) of 41 mL/min/kg. In C57BL/6 mice, YQ128 (10 mg/kg) has been shown to trigger IL-1β production in a NLRP3- dependent manner . |
分子量 | 545.11 |
分子式 | C27H29ClN2O4S2 |
CAS No. | 2454246-18-3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 248 mg/mL (454.95 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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