| Identification | Back Directory | [Name]
LMT-28 | [CAS]
1239600-18-0 | [Synonyms]
LMT-28
LMT-28 >=98% (HPLC)
2-Oxazolidinone, 3-[(2S,3S)-3-hydroxy-2-methyl-4-methylene-1-oxononyl]-4-(1-methylethyl)-, (4S)- | [Molecular Formula]
C17H29NO4 | [MDL Number]
MFCD30187587 | [MOL File]
1239600-18-0.mol | [Molecular Weight]
311.42 |
| Chemical Properties | Back Directory | [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), | [form ]
oil | [pka]
13.97±0.20(Predicted) | [color ]
colorless to light yellow, oil | [Water Solubility ]
< 0.1 mg/mL Water (insoluble) | [InChI]
1S/C17H29NO4/c1-6-7-8-9-12(4)15(19)13(5)16(20)18-14(11(2)3)10-22-17(18)21/h11,13-15,19H,4,6-10H2,1-3,5H3/t13-,14+,15+/m0/s1 | [InChIKey]
UDXWSYOXIRPYFK-RRFJBIMHSA-N | [SMILES]
CC(C)[C@H](N1C([C@@H](C)[C@H](O)C(CCCCC)=C)=O)COC1=O |
| Hazard Information | Back Directory | [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%.
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| [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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| Company Name: |
Sigma-Aldrich
|
| Tel: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|