TJ-M2010-5 是一种MyD88抑制剂,可与 MyD88 的 TIR 结构域结合以干扰其同源二聚化和 TLR/MyD88 信号通路。TJ-M2010-5 可用于心肌缺血/再灌注损伤(MIRI)的研究。
生物活性 | TJ-M2010-5 is aMyD88inhibitor that binds to the TIR domain ofMyD88to interfere with its homodimerization, and the TLR/MyD88 signal pathway[1][2]. TJ-M2010-5 can be used for the research of myocardial ischemia/reperfusion injury (MIRI)[2]. |
体外研究 (In Vitro) | TJ-M2010-5 (40 μM) inhibits MyD88 homodimerization in transfected HEK293 cells in a concentration-dependent manner and suppresses MyD88 signaling in LPS (100 ng/mL)-responsive RAW 264.7 cells in vitro[1]. TJ-M2010-5 (5-30 μM) prevents B cell proliferation and induces B cells apoptosis after stimulation with R848 (500 ng/mL)[3].
Cell Viability Assay[3] Cell Line: | Purified B cells | Concentration: | 0 μM, 5 μM, 10 μM, 20 μM and 30 μM | Incubation Time: | 48 hours | Result: | Inhibited the viability of B cells with or without the stimulation of CD40L. |
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体内研究 (In Vivo) | TJ-M2010-5 treatment statistically significantly reduces AOM/DSS-induced colitis and completely prevented CAC development with less related body mass loss, results in 0% mortality of treated mice, decreases cell proliferation, and increased apoptosis in colon tissue in a 10-week CAC mouse model[1]. TJ-M2010-5 statistically significantly decreases TNF-α, IL-6, G-CSF, MIP-1β, IL-11, IL-17A, IL-22, and IL-23 serum concentrations in mice at both two and seven weeks postinduction, as well as TGF-β1 serum levels at seven weeks postinduction[1].
Animal Model: | Female BalB/c mice (6–8 weeks old)[1] | Dosage: | 50 mg/kg | Administration: | Treated i.p. daily beginning two days before the first dextran sodium sulfate (DSS) administration throughout a 10-week observation period. | Result: | Significantly prevented inflammation/CAC-related body weight loss and mortality (0% vs 53% in the control group). |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen) |
溶解性数据 | In Vitro: DMSO : 100 mg/mL(245.98 mM;Need ultrasonic) 配制储备液 1 mM | 2.4598 mL | 12.2989 mL | 24.5978 mL | 5 mM | 0.4920 mL | 2.4598 mL | 4.9196 mL | 10 mM | 0.2460 mL | 1.2299 mL | 2.4598 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 (protect from light, stored under nitrogen)。-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: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.15 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (6.15 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (6.15 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 25.0 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。 *以上所有助溶剂都可在本网站选购。
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