LMT-28|cas:1239600-18-0|西域试剂

LMT-28,98.06%

产品编号：Bellancom-102084| CAS NO：1239600-18-0| 分子式：C₁₇H₂₉NO₄| 分子量：311.42

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货号	价格	库存与货期
Bellancom-102084	￥800.00	杭州北京（现货）
Bellancom-102084	￥1400.00	杭州北京（现货）
Bellancom-102084	￥3000.00	杭州北京（现货）
Bellancom-102084	￥5000.00	杭州北京（现货）
Bellancom-102084	￥8500.00	杭州北京（现货）

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LMT-28

产品介绍

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 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.

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

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
(In Vivo)

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.

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

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%.

体内研究

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

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%.

体内研究

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

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%.

性状

Oil

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。
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
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。
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
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。