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YQ128
CAS No. 2454246-18-3
YQ128 ( —— )
产品货号. M26514 CAS No. 2454246-18-3
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。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 2MG | ￥616 | 有现货 |
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| 5MG | ￥1026 | 有现货 |
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| 10MG | ￥1596 | 有现货 |
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| 25MG | ￥3004 | 有现货 |
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| 50MG | ￥4306 | 有现货 |
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| 100MG | ￥5832 | 有现货 |
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| 500MG | ￥11610 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
| 1 mL x 10 mM in DMSO | ￥1226 | 有现货 |
|
生物学信息
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产品名称YQ128
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注意事项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
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产品简述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。
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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.(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 .
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体外实验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.
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体内实验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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同义词——
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通路Apoptosis
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靶点IL Receptor
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受体M5 mAChR
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研究领域——
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适应症——
化学信息
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CAS Number2454246-18-3
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分子量545.11
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分子式C27H29ClN2O4S2
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纯度>98% (HPLC)
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溶解度In Vitro:?DMSO : 250 mg/mL (458.62 mM)
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SMILESCCCOc1ccc(Cl)cc1CN(CCc1ccc(cc1)S(=O)(=O)NCC#C)C(=O)Cc1ccsc1
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
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MyD88-IN-1
MyD88-IN-1 是一种有效的 MyD88 抑制剂。MyD88-IN-1 抑制 TLR4 和 MyD88 的相互作用并抑制 NF-κB 通路。MyD88-IN-1 可用于癌症和炎症的研究。
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NFAT inhibitor, Cell...
NFAT inhibitor. Inhibits LPS or LPS plus IFN-γ-induced IL-12 p40, IL-12 p70, IL-23 and TNF secretion from bone marrow-derived macrophages (BMDMs). Also attenuates NO production and Nos2 mRNA expression in LPS-stimulated BMDMs. Improves symptoms in a mouse model of colitis. Exhibits immunosuppressive effects; enhances graft survival in mice. Cell permeable.
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ABzOH
ABzOH is a benzoic acid derivative, similar in structure to non-steroidal anti-inflammatory drugs such as aspirin, with anti-inflammatory, anti-tumor and anti-proliferative effects. ABzOH can not only inhibit the expression of tumor necrosis factor-α (TNF-a), interleukin-1β (IL-1β), interleukin-6 (IL-6) and other pro-inflammatory cytokines, but also inhibit breast cancer, lung cancer and pancreatic cancer.
