產(chǎn)品描述: | JTE-607, a highly selective inflammatory cytokine synthesis inhibitor, protects from endotoxin shock in mice. JTE-607 inhibits inflammatory cytokine production, including TNF-α, IL-1β, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC50s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively. Cleavage and Polyadenylation Specificity Factor 3 (CPSF3) is the target of JTE-607 |
靶點(diǎn): |
IL-10;IL-6;IL-8;CysteineProtease |
體外研究: |
JTE-607 抑制 LPS 刺激的人 PBMC 產(chǎn)生炎癥細(xì)胞因子,包括 TNF-α、IL-1β、IL-6、IL-8 和 IL-10,IC50 分別為 11,5.9、8.8、7.3 和 9.1 nM。JTE-607 的抑制作用也見于這些細(xì)胞因子的 mRNA 表達(dá)。 JTE-607 抑制 LPS 刺激的人 PBMC 產(chǎn)生炎性細(xì)胞因子的 IC50 大約 10 nM。 JTE607 抑制猴和兔 PBMC 中 LPS 刺激的 IL-8 產(chǎn)生,以及小鼠和大鼠 PBMC 中 TNF-α 的產(chǎn)生,IC50 分別為 59、780、1600 和 19000 nM。 JTE607 還抑制其他細(xì)胞因子,粒細(xì)胞-巨噬細(xì)胞集落刺激因子和 IL-1RA,IC50 分別為 2.4±0.8 和 5.4±0.4 nM。 JTE-607 抑制猴、兔、小鼠和大鼠細(xì)胞因子的產(chǎn)生,IC50 分別為 59±26、780±120、1600±650 和 19000±3200 nM。 RT-PCR Cell Line: human peripheral blood mononuclear cells (PBMCs) Concentration: 100 nM Incubation Time: 20 hours Result: Reduced the increase in the level of mRNAs of TNF-α, IL-1b, IL-6 and IL-8. |
體內(nèi)研究: |
JTE-607 (0.3-10 mg/kg,iv) 在 C. parvum 敏感小鼠中劑量依賴性地降低 LPS 攻擊后的死亡率,同時(shí)小鼠血漿中 TNF-α 降低。 Animal Model: Male C57BL/6 mice (5 to 6 weeks old) are sensitized by injecting Corynebacterium parvum Dosage: 0.3, 1, 3, 10 mg/kg Administration: Administered intravenously 10 min before the LPS challenge. Result: Showed dose dependent inhibition of the mortality at 0.3 to 10 mg/kg and significant effect at 3 and 10 mg/kg. |
參考文獻(xiàn): |
1. M Kakutani, et al. JTE-607, a novel inflammatory cytokine synthesis inhibitor without immunosuppression, protects from endotoxin shock in mice. Inflamm Res. 1999 Aug;48(8):461-8. 2. Nathan T Ross, et al. CPSF3-dependent pre-mRNA processing as a druggable node in AML and Ewing's sarcoma. Nat Chem Biol. 2020 Jan;16(1):50-59. |
溶解性: |
Soluble in DMSO、H2O |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
1.907 ml |
9.534 ml |
19.068 ml |
5 mM |
0.381 ml |
1.907 ml |
3.814 ml |
10 mM |
0.191 ml |
0.953 ml |
1.907 ml |
50 mM |
0.038 ml |
0.191 ml |
0.381 ml |
|
注意: |
部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。 |