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1239600-18-0

中文名稱 LMT-28
CAS 1239600-18-0
分子式 C17H29NO4
分子量 311.42
MOL 文件 1239600-18-0.mol
1239600-18-0 結(jié)構(gòu)式 1239600-18-0 結(jié)構(gòu)式

基本信息

中文別名
(4S)-3-[(2S,3S)-3-羥基-2-甲基-4-亞甲基-1-氧代癸烷基]-4-(1-甲基乙基)-2-惡唑烷酮
英文別名
LMT-28
LMT-28 >=98% (HPLC)
2-Oxazolidinone, 3-[(2S,3S)-3-hydroxy-2-methyl-4-methylene-1-oxononyl]-4-(1-methylethyl)-, (4S)-

物理化學(xué)性質(zhì)

儲存條件-20°C
形態(tài)oil
顏色無色至淡黃色

常見問題列表

生物活性
LMT-28 是一種具有口服活性的通過直接與 gp130 結(jié)合而發(fā)揮作用的 IL-6 抑制劑。LMT-28 具有低毒性,并選擇性抑制 IL-6 誘導(dǎo)的 STAT3、JAK2 和 gp130 的磷酸化。
靶點

IL-6

體外研究

LMT-28 reduces IL-6-induced luciferase activity by ~90% at a concentration of 50 μM and exhibits an IC 50 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.
體內(nèi)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%.
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