LMT-28
LMT-28 Basic information
- Product Name:
- LMT-28
- Synonyms:
-
- LMT-28
- 2-Oxazolidinone, 3-[(2S,3S)-3-hydroxy-2-methyl-4-methylene-1-oxononyl]-4-(1-methylethyl)-, (4S)-
- LMT-28 >=98% (HPLC)
- LMT28,LMT 28
- LMT-28, 10 mM in DMSO
- (S)-3-((2S,3S)-3-Hydroxy-2-methyl-4-methylenenonanoyl)-4-isopropyloxazolidin-2-one
- CAS:
- 1239600-18-0
- MF:
- C17H29NO4
- MW:
- 311.42
- Mol File:
- 1239600-18-0.mol
LMT-28 Chemical Properties
- Boiling point:
- 452.9±38.0 °C(Predicted)
- Density
- 1.065±0.06 g/cm3(Predicted)
- storage temp.
- -20°C
- solubility
- 100 mg/mL in DMSO (321.11 mM),
- pka
- 13.97±0.20(Predicted)
- form
- oil
- color
- colorless to light yellow, oil
- Water Solubility
- < 0.1 mg/mL Water (insoluble)
LMT-28 Usage And Synthesis
Uses
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[1].
Biochem/physiol Actions
LMT-28 is a derivative of oxazolidinone. It has the ability to repress the activation of signal transducer and activator of transcription 3 (STAT3) stimulated by interleukin 6 (IL-6). Orally administered LMT-28 reduced arthritis and acute pancreatitis stimulated by collagen in mice pathologic models.
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%. |
IC 50
IL-6
References
[1] Hong SS, et al. A Novel Small-Molecule Inhibitor Targeting the IL-6 Receptor β Subunit, Glycoprotein 130. J Immunol. 2015 Jul 1;195(1):237-45. DOI:10.4049/jimmunol.1402908
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