YQ128

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

YQ128是第二代NLRP3（NOD样受体P3）炎症小体的有效选择性抑制剂（IC50为0.30 μM），具有抗炎活性。

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.(In Vitro):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). (In Vivo):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 .

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. 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.

YQ128 (iv; 20 mg/kg) has an intermediate terminal plasma half-life (t1/2) of 6.6 hours after iv administration. YQ128 (oral; 20 mg/kg) shows delayed gastrointestinal absorption with a tmax and cmax of 12 h and 73 ng/mL, respectively. Oral bioavailability (Foral) is estimated as 10%. YQ128 exhibits extensive extravascular distribution with a large steady-state volume of distribution (Vdss) of 8.5 L/kg and rapid total clearance (CLtot) 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. Animal Model:Sprague-Dawley rats (200-250 g)Dosage:20 mg/kg (Pharmacokinetic Analysis)Administration:Iv Result:Had an intermediate terminal plasma half-life (t1/2) of 6.6 hours after iv administration.

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Apoptosis

IL Receptor

M5 mAChR

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2454246-18-3

545.11

C27H29ClN2O4S2

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (458.62 mM)

CCCOc1ccc(Cl)cc1CN(CCc1ccc(cc1)S(=O)(=O)NCC#C)C(=O)Cc1ccsc1

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(-20℃)

With Ice Pack

≥ 2 years