JTE-607|188791-09-5|(甲氧番荔枝碱)-陌孚医药/Medlife

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JTE-607 (Synonyms: 甲氧番荔枝碱)

目录号: PL13370 纯度: ≥98%

CAS No. :188791-09-5

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中文名称	JTE-607
中文别名	甲氧番荔枝碱
英文名称	JTE-607
英文别名	N-[3,5-Dichloro-2-hydroxy-4-[2-(4-methyl-1-piperazinyl)ethoxy]benzoyl]-L-phenylalanine ethyl ester dihydrochloride;JTE-607;ethyl (2S)-2-[[3,5-dichloro-2-hydroxy-4-[2-(4-methylpiperazin-1-yl)ethoxy]benzoyl]amino]-3-phenylpropanoate,dihydrochloride;JTE 607 dihydrochloride;JTE607Dihydrochloride;JTE 607;2B68H6BWCX;ethyl (2S)-2-[[3,5-dichloro-2-hydroxy-4-[2-(4-methylpiperazin-1-yl)ethoxy]benzoyl]amino]-3-phenylpropanoate;dihydrochloride;(-)-ethyl N-(3,5-dichloro-2-hydroxy-4-(2-(4-methylpiperazin-1-yl))ethoxybenzoyl)-L-phenylamine dihydrochloride
Cas No.	188791-09-5
分子式	C₂₅H₃₃Cl₄N₃O₅
分子量	597.36
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	JTE-607 是一种高选择性的炎性细胞因子合成抑制剂，可保护小鼠免受内毒素休克。JTE-607 作用于 LPS 刺激的人 PBMC，抑制 TNF-α、IL-1β、IL-6、IL-8 和 IL-10 的 IC₅₀ 分别为 11、5.9、8.8、7.3 和 9.1 nM。断裂和聚腺苷酸化特异因子 3 (CPSF3) 是 JTE-607的靶蛋白。
生物活性	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 IC 50 s 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.
性状	Solid
体外研究(In Vitro)	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. The inhibitory effects of JTE-607 are also seen in mRNA expression of those cytokines. JTE-607 inhibits inflammatory cytokine production from LPS-stimulated human PBMCs with an IC50 of approximately 10 nM. JTE607 inhibits LPS-stimulated IL-8 production from monkey and rabbit PBMCs, and TNF-α production from mouse and rat PBMCs with IC50s of 59, 780, 1600 and 19000 nM, respectively. JTE607 also suppresses other cytokines, granulocyte-macrophage colony stimulating factor and IL-1RA with IC50s of 2.4±0.8 and 5.4±0.4 nM, respectively. JTE-607 inhibits cytokine production in monkey, rabbit, mouse and rat with IC50s of 59±26
体内研究(In Vivo)	JTE-607 (0.3-10 mg/kg, i.v.) shows dose dependent inhibition of mortality after LPS challenge in C. parvum sensitized mice in accordance with a decrease of plasma TNF-α. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[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 Ewings sarcoma. Nat Chem Biol. 2020 Jan;16(1):50-59.

溶解度数据	In Vitro: DMSO : 250 mg/mL (418.51 mM; Need ultrasonic)H₂O : 20 mg/mL (33.48 mM; ultrasonic and warming and heat to 60°C)配制储备液

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