| 生物活性 | JTE-607, a highly selectiveinflammatory cytokine synthesisinhibitor, protects from endotoxin shock in mice. JTE-607 inhibits inflammatory cytokine production, includingTNF-α,IL-1β,IL-6,IL-8andIL-10, from LPS-stimulated human PBMCs, withIC50s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively[1]. Cleavage and Polyadenylation Specificity Factor 3 (CPSF3) is the target of JTE-607[2]. |
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[1].
JTE-607 inhibits inflammatory cytokine production from LPS-stimulated human PBMCs with an IC50of approximately 10 nM[1].
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[1].
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[1].
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[1].
RT-PCR[1] | 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. |
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体内研究
(In Vivo) | JTE-607 (0.3-10 mg/kg, i.v.) shows dose dependent inhibition of mortality after LPS challenge inC. parvumsensitized mice in accordance with a decrease of plasma TNF-α[1].
| Animal Model: | Male C57BL/6 mice (5 to 6 weeks old) are sensitized by injectingCorynebacterium parvum[1] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 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℃) 配制储备液 | 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 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。 *以上所有助溶剂都可在本网站选购。
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