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LMT-28 is a novel and potent IL-6 blocker, acting by inhibiting IL-6Rβ (gp130) with IC50 of 5.9 uM (IL-6–induced luciferase activity), selectively inhibiting IL-6–induced phosphorylation of STAT3, JAK2, and gp130.
| ln Vitro |
At 50 μM, LMT-28 has an IC50 value of 5.9 μM and can inhibit IL-6-induced luciferase activity by almost 90%. LMT-28 (1–100 μM; 1 hour) specifically inhibits IL-6-induced STAT3, JAK2, and gp130 [1]. Cell erythroid cell line TF-1 phosphorylation is inhibited by LMT-28 (1–100 μM; 72 hours) in relation to IL-6-induced phosphorylation of human tissue.
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| ln Vivo |
CIA is attenuated by LMT-28 (0-0.5 mg/kg; applied topically once daily for 15 days)[1]. LMT-28 simulates the development of face inflammation (0.25 or 1 mg/kg; po). By directly binding to gp130, the -28 bridge inhibits gp130's reaction to the IL-6/IL-6Rα combination [1].
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| Cell Assay |
Cell proliferation analysis [1] Cell erythroid cell line TF-1 phosphorylation [1].
Cell Types: TF-1 cells (1 ng/mL IL-6 induced) Tested Concentrations: 1, 10, 100, 1000, 10000 nM Incubation Duration: 72 hrs (hours) Experimental Results: Dramatically inhibited IL-6-induced TF-1 proliferation, IC50 The value is 7.5 μM. Western Blot Analysis[1] Cell Types: HepG2 cells (treated with 10 ng/mL IL-6) Tested Concentrations: 1, 3, 10, 30 and 100 μM Incubation Duration: 1 hour Experimental Results: Inhibition of IL-6-induced phosphorylated STAT3 , JAK2 and gp130. |
| Animal Protocol |
Animal/Disease Models: Sixweeks old male DBA/1J mice (collagen-induced arthritis mice, CIA) [1]
Doses: 0-0.5 mg/kg Route of Administration: Oral; one time/day for 15 days Experimental Results: Serum cartilage Oligomeric matrix protein (COMP) levels were Dramatically diminished by 50%, serum amyloid P (SAP) levels were Dramatically diminished by 55%, and anti-CII IgG levels were Dramatically diminished by 62%. |
| References |
| Molecular Formula |
C17H29NO4
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|---|---|
| Molecular Weight |
311.42
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| Exact Mass |
311.209
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| CAS # |
1239600-18-0
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| PubChem CID |
49846977
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| Appearance |
Colorless to light yellow viscous liquid
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
452.9±38.0 °C at 760 mmHg
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| Flash Point |
227.7±26.8 °C
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| Vapour Pressure |
0.0±2.5 mmHg at 25°C
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| Index of Refraction |
1.493
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| LogP |
3.05
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
22
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| Complexity |
419
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| Defined Atom Stereocenter Count |
3
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| SMILES |
O1C(N(C([C@@H](C)[C@@H](C(=C)CCCCC)O)=O)[C@H](C1)C(C)C)=O
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| InChi Key |
UDXWSYOXIRPYFK-RRFJBIMHSA-N
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| InChi Code |
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
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| Chemical Name |
(4S)-3-[(2S,3S)-3-hydroxy-2-methyl-4-methylidenenonanoyl]-4-propan-2-yl-1,3-oxazolidin-2-one
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| Synonyms |
LMT28 LMT 28 LMT-28
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~321.11 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (8.03 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (8.03 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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