| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S89270-5mg促销 |
≥97% | ￥800.00 ￥720.00 |
10 | - | - | - | - |
|
S89270-10mg促销 |
≥97% | ￥1160.00 ￥1050.00 |
8 | - | - | - | - |
|
S89270-25mg促销 |
≥97% | ￥2330.00 ￥2100.00 |
3 | - | - | - | - |
|
S89270-50mg促销 |
≥97% | ￥3590.00 ￥3230.00 |
2 | - | - | - | - |
|
S89270-100mg促销 |
≥97% | ￥5750.00 ￥5180.00 |
4 | - | - | - | - |
|
S89270-200mg促销 |
≥97% | ￥8990.00 ￥8090.00 |
2 | - | - | - | - |
|
| 产品描述： | JH-X-119-01 is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 ameliorates LPS-induced sepsis in mice. JH-X-119-01 inhibits IRAK1 biochemically with an apparent IC50 of 9 nM while exhibiting no inhibition of IRAK4 at concentrations up to 10 μM | ||||||||||||||||||||
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| 靶点： | IRAK-1:9 nM (IC50);IRAK | ||||||||||||||||||||
| 体外研究： | JH-X-119-01 (10 μM) decreases phosphorylation of NF-κB and mRNA levels of IL-6 and TNFα in LPS-treated macrophages in vitro. JH-X-119-01 selectively inhibits IRAK1 phosphorylation. JH-X-119-01 exhibits off-target inhibition of only two additional kinases, YSK4 and MEK3. Dose response analysis reveals an IC50 of 57 nM for YSK4[2]. JH-X-119-01 shows moderate cell killing effects in a panel of Waldenström’s macroglobulinemia (WM) cells, Diffused Large B-cell Lymphoma (DLBCL) cells, and lymphoma cells expressing mutant MYD88, with EC50s ranging from 0.59 to 9.72 μM. Western Blot Analysis Cell Line: RAW 264.7 cells and THP-1 cells Concentration: 10 μM Incubation Time: 15 minutes Result: Decreased LPS (100 ng/mL)-induced phosphorylation of IκBα and NF-κB-P65. | ||||||||||||||||||||
| 体内研究： | JH-X-119-01 improves survival and decreases immunopathies of LPS-challenged mice. JH-X-119-01 increases survival of mice at the dose of 5 mg/kg body weight. Survival is further improved when the dose is increased to 10 mg/kg. Animal Model: C57BL/6 (20-22 g, male) mice Dosage: 5 mg/kg and 10 mg/kg Administration: Intraperitoneally injected; 5 days Result: Protected mice from LPS (20 mg/kg)-induced sepsis. Survival at day 5 was 13.3% in control group where septic mice were treated by vehicle, while the values were 37.5% and 56.3% for 5 mg/kg and 10 mg/kg. | ||||||||||||||||||||
| 参考文献： | 1. Bin Pan, et al. Selective inhibition of interleukin-1 receptor-associated kinase 1 ameliorates lipopolysaccharide-induced sepsis in mice. Int Immunopharmacol. 2020 Aug;85:106597. 2. John M Hatcher, et al. Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma. ACS Med Chem Lett. 2020 Oct 9;11(11):2238-2243. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
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危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京