LMT-28 是一种具有口服活性的通过直接与 gp130 结合而发挥作用的IL-6抑制剂。LMT-28 具有低毒性，并选择性抑制 IL-6 诱导的 STAT3、JAK2 和 gp130 的磷酸化。
| 生物活性 | LMT-28 is an orally active and the first syntheticIL-6inhibitor that functions through direct binding to gp130. LMT-28 shows low toxicity and selectively inhibits IL-6-induced phosphorylation ofSTAT3,JAK2, and gp130[1]. |
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体外研究
(In Vitro) | LMT-28 reduces IL-6-induced luciferase activity by ~90% at a concentration of 50 μM and exhibits an IC50value of 5.9 μM. LMT-28 (1-10 μM; 72 hours) inhibits IL-6-induced proliferation of the human erythroleukemic cell line TF-1[1].
LMT-28 (1-100 μM; 1 hour) selectively inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130[1].
Cell Proliferation Assay[1] | Cell Line: | TF-1 cells (1 ng/mL IL-6-induced) | | Concentration: | 1, 10, 100, 1000, 10000 nM | | Incubation Time: | 72 hours | | Result: | Markedly inhibited IL-6–induced TF-1 proliferation with an IC50 value of 7.5 μM. |
Western Blot Analysis[1] | Cell Line: | HepG2 cells (treated with 10 ng/mL IL-6) | | Concentration: | 1, 3, 10, 30, and 100 μM | | Incubation Time: | 1 hour | | Result: | Inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130. |
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体内研究
(In Vivo) | LMT-28 (0-0.5 mg/kg; p.o.; once daily for 15 days) alleviates CIA in mice[1].
LMT-28 (0.25 or 1 mg/kg; p.o.) ameliorates the progression of pancreatitis in mice. LMT-28 binds directly and specifically to gp130, and thereby inhibits the interaction of gp130 with the IL-6/IL-6Rα complex[1].
| Animal Model: | Six-week-old male DBA/1J mice (collagen-induced arthritis mice, CIA)[1] | | Dosage: | 0-0.5 mg/kg | | Administration: | Oral; once daily for 15 days | | Result: | Markedly reduced the serum levels of cartilage oligomeric matrix protein (COMP) by 50%, serum amyloid P (SAP) by 55%, and anti-CII IgG by 62%. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Pure form | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(321.11 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.2111 mL | 16.0555 mL | 32.1110 mL | | 5 mM | 0.6422 mL | 3.2111 mL | 6.4222 mL | | 10 mM | 0.3211 mL | 1.6055 mL | 3.2111 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。-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 (8.03 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (8.03 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 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 (8.03 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (8.03 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。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (8.03 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.03 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 25.0 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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