LMT-28
目录号 : KM2420 CAS No. : 1239600-18-0 纯度 : 98%

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。

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5mg
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25mg
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50mg
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100mg
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200mg 询价 In-stock
500mg 询价 In-stock

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生物活性

LMT-28 is an orally active and the first synthetic IL-6 inhibitor that functions through direct binding to gp130. LMT-28 shows low toxicity and selectively inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130.

体外研究

LMT-28 reduces IL-6-induced luciferase activity by ~90% at a concentration of 50 μM and exhibits an IC50 value of 5.9 μM. LMT-28 (1-10 μM; 72 hours) inhibits IL-6-induced proliferation of the human erythroleukemic cell line TF-1.
LMT-28 (1-100 μM; 1 hour) selectively inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130.

Cell Proliferation Assay

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

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.
体内研究

LMT-28 (0-0.5 mg/kg; p.o.; once daily for 15 days) alleviates CIA in mice.
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.

Animal Model: Six-week-old male DBA/1J mice (collagen-induced arthritis mice, CIA)
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%.
分子式
C17H29NO4
分子量
311.42
CAS号
1239600-18-0
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
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (321.11 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-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: 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-CD in 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 μL 20% 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。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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