JTE-607 甲氧番荔枝碱|cas:188791-09-5|西域试剂

JTE-607 甲氧番荔枝碱,98.42%

产品编号：Bellancom-110133| CAS NO：188791-09-5| 分子式：C₂₅H₃₃Cl₄N₃O₅| 分子量：597.36

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-110133	￥1000.00	杭州北京（现货）
Bellancom-110133	￥1800.00	杭州北京（现货）
Bellancom-110133	￥3800.00	杭州北京（现货）
Bellancom-110133	￥6500.00	杭州北京（现货）
Bellancom-110133	￥10800.00	杭州北京（现货）

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JTE-607 甲氧番荔枝碱

产品介绍

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 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.

体外研究

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, 780±120, 1600±650 and 19000±3200 nM, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

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

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6740 mL	8.3702 mL	16.7403 mL
5 mM	0.3348 mL	1.6740 mL	3.3481 mL
10 mM	0.1674 mL	0.8370 mL	1.6740 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： PBS
Solubility: 100 mg/mL (167.40 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.48 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.48 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.48 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.48 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.48 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.48 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。